Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL411 (Apstil, Cyren a, Diethylstilbestrol, Distilbene, Estrobene, Estrogenine, Estromenin, Fonatol, New-estranol 1, NSC-3070, Palestrol, Stilbestro, Stilbestroform, Stilbestrol, Stilbetin, Stilboesterol, Stilboestrol, Synestrin, Synthestrin, Tampovagan) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303] | ||||||||
ChEMBL | DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine) | B | 4.59 | pIC50 | 25550 | nM | IC50 | DrugMatrix in vitro pharmacology data |
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
ChEMBL | DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) | B | 5.78 | pKi | 1666 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) | B | 5.54 | pIC50 | 2856 | nM | IC50 | DrugMatrix in vitro pharmacology data |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
ChEMBL | DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) | B | 5.3 | pKi | 5060 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) | B | 5.05 | pIC50 | 9013 | nM | IC50 | DrugMatrix in vitro pharmacology data |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
ChEMBL | DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) | B | 5.9 | pKi | 1248 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) | B | 5.66 | pIC50 | 2208 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 5.1 | pKi | 7888 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 4.71 | pIC50 | 19487 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 5.27 | pKi | 5321 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 4.97 | pIC50 | 10826 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 5.28 | pKi | 5297 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 4.85 | pIC50 | 14127 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 5.27 | pKi | 5340 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 4.93 | pIC50 | 11698 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 5.66 | pKi | 2201 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 4.82 | pIC50 | 15151 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207] | ||||||||
ChEMBL | Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) | B | 4.85 | pIC50 | 14125.38 | nM | IC50 | J Med Chem (2005) 48: 5666-5674 [PMID:16134935] |
Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530] | ||||||||
ChEMBL | DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) | B | 5.53 | pIC50 | 2963 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
ChEMBL | TP_TRANSPORTER: drug resistance(Mitoxantrone) in BCRP-expressing K562 cells | F | 6.3 | pIC50 | 500 | nM | IC50 | Mol Cancer Ther (2003) 2: 105-112 [PMID:12533678] |
ChEMBL | TP_TRANSPORTER: drug resistance(SN-38) in BCRP-expressing K562 cells | F | 6.3 | pIC50 | >500 | nM | IC50 | Mol Cancer Ther (2003) 2: 105-112 [PMID:12533678] |
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
ChEMBL | DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) | B | 4.89 | pKi | 12755 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) | B | 4.66 | pIC50 | 22088 | nM | IC50 | DrugMatrix in vitro pharmacology data |
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219] | ||||||||
ChEMBL | DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) | B | 5.25 | pIC50 | 5600 | nM | IC50 | DrugMatrix in vitro pharmacology data |
CysLT1 receptor/Cysteinyl leukotriene receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1798] [GtoPdb: 269] [UniProtKB: Q9Y271] | ||||||||
ChEMBL | DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4) | B | 5.05 | pKi | 8872 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4) | B | 4.75 | pIC50 | 17745 | nM | IC50 | DrugMatrix in vitro pharmacology data |
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
ChEMBL | DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) | B | 6.02 | pKi | 958 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) | B | 5.57 | pIC50 | 2718 | nM | IC50 | DrugMatrix in vitro pharmacology data |
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
ChEMBL | DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) | B | 5.41 | pKi | 3882 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) | B | 5.11 | pIC50 | 7763 | nM | IC50 | DrugMatrix in vitro pharmacology data |
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) | B | 5.35 | pKi | 4440 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) | B | 4.88 | pIC50 | 13321 | nM | IC50 | DrugMatrix in vitro pharmacology data |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 5.52 | pKi | 2987 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 5.06 | pIC50 | 8796 | nM | IC50 | DrugMatrix in vitro pharmacology data |
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
ChEMBL | DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 6.07 | pKi | 851 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.97 | pIC50 | 1071 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] | ||||||||
ChEMBL | In vitro displacement of 0.5 nM [3H]17-beta-estradiol from human Estrogen receptor alpha | B | 9.31 | pKi | 0.49 | nM | Ki | J Med Chem (2003) 46: 1408-1418 [PMID:12672240] |
ChEMBL | DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol) | B | 9.58 | pKi | 0.26 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of [3H]Estradiol from human recombinant estrogen receptor alpha expressed in Sf9 cells after 2 hrs | B | 9.66 | pKi | 0.22 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
GtoPdb | - | - | 10.4 | pKi | - | - | - | Endocrinology (1997) 138: 863-70 [PMID:9048584] |
ChEMBL | Displacement of [3H]-estradiol from human recombinant ERalpha expressed in Sf21 cells after 2 hrs | B | 6.11 | pIC50 | 770 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4307-4309 [PMID:22652053] |
ChEMBL | In vitro inhibition of [3H]17-beta-estradiol binding to human estrogen receptor alpha | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2001) 44: 1654-1657 [PMID:11356100] |
ChEMBL | DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol) | B | 9.04 | pIC50 | 0.92 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of [3H]Estradiol from human recombinant estrogen receptor alpha expressed in Sf9 cells after 2 hrs | B | 9.11 | pIC50 | 0.77 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
ChEMBL | Displacement of radioligand from Estrogen receptor alpha | B | 9.48 | pIC50 | 0.33 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1283-1285 [PMID:11965371] |
ChEMBL | Inhibition of [3H]17-beta-estradiol binding to human recombinant Estrogen receptor alpha. | B | 7.92 | pEC50 | 12 | nM | EC50 | J Med Chem (2002) 45: 1399-1401 [PMID:11906280] |
ChEMBL | Agonist activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ER-alpha-mediated transcriptional activity by luciferase reporter gene assay | B | 9.7 | pEC50 | 0.2 | nM | EC50 | Bioorg Med Chem (2019) 27: 1952-1961 [PMID:30940565] |
ChEMBL | Selective estrogen receptor down-regulator activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ERalpha degradation by luciferase reporter gene assay | B | 9.96 | pEC50 | 0.11 | nM | EC50 | Bioorg Med Chem (2019) 27: 1952-1961 [PMID:30940565] |
ChEMBL | Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor alpha. | B | 10.22 | pEC50 | 0.06 | nM | EC50 | J Med Chem (2002) 45: 1399-1401 [PMID:11906280] |
Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731] | ||||||||
ChEMBL | In vitro displacement of 0.5 nM [3H]17-beta-estradiol from human Estrogen receptor beta | B | 9.2 | pKi | 0.63 | nM | Ki | J Med Chem (2003) 46: 1408-1418 [PMID:12672240] |
GtoPdb | - | - | 9.8 | pKi | - | - | - | Endocrinology (1997) 138: 863-70 [PMID:9048584] |
ChEMBL | Displacement of [3H]-estradiol from human recombinant ERbeta expressed in Sf21 cells after 2 hrs | B | 6.21 | pIC50 | 610 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4307-4309 [PMID:22652053] |
ChEMBL | In vitro inhibitory concentration against [3H]17-beta-estradiol binding to human estrogen receptor 2 | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2001) 44: 1654-1657 [PMID:11356100] |
ChEMBL | Inhibition of [3H]17-beta-estradiol binding to human recombinant Estrogen receptor beta. | B | 8.05 | pEC50 | 9 | nM | EC50 | J Med Chem (2002) 45: 1399-1401 [PMID:11906280] |
ChEMBL | Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor beta. | B | 10.7 | pEC50 | 0.02 | nM | EC50 | J Med Chem (2002) 45: 1399-1401 [PMID:11906280] |
Estrogen-related receptor-γ/Estrogen-related receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4245] [GtoPdb: 624] [UniProtKB: P62508] | ||||||||
GtoPdb | - | - | 5.3 | pIC50 | - | - | - |
Genes Dev (2001) 15: 833-8 [PMID:11297507]; Proc Natl Acad Sci USA (2001) 98: 8880-4 [PMID:11447273] |
ChEMBL | Estrogen-Related Receptor gamma activity in FRET assay | F | 6.2 | pEC50 | 630 | nM | EC50 | J Med Chem (2005) 48: 3107-3109 [PMID:15857113] |
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] | ||||||||
ChEMBL | DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) | B | 5.32 | pKi | 4818 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) | B | 4.97 | pIC50 | 10600 | nM | IC50 | DrugMatrix in vitro pharmacology data |
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
ChEMBL | DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 5.74 | pKi | 1825 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 5.34 | pIC50 | 4563 | nM | IC50 | DrugMatrix in vitro pharmacology data |
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
ChEMBL | DRUGMATRIX: Protein Serine/Threonine Kinase, p38alpha enzyme inhibition (substrate: Myelin Basic Protein) | B | 4.48 | pIC50 | 32903 | nM | IC50 | DrugMatrix in vitro pharmacology data |
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
ChEMBL | DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 5.63 | pKi | 2345 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 5.24 | pIC50 | 5778 | nM | IC50 | DrugMatrix in vitro pharmacology data |
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
ChEMBL | DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 5.44 | pKi | 3654 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 4.82 | pIC50 | 15171 | nM | IC50 | DrugMatrix in vitro pharmacology data |
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
ChEMBL | DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 5.41 | pKi | 3907 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 4.73 | pIC50 | 18432 | nM | IC50 | DrugMatrix in vitro pharmacology data |
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452] | ||||||||
ChEMBL | DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) | B | 5.5 | pKi | 3184 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) | B | 5.02 | pIC50 | 9553 | nM | IC50 | DrugMatrix in vitro pharmacology data |
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.44 | pKi | 3640 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.44 | pIC50 | 3670 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469] | ||||||||
ChEMBL | Antagonist activity at full length human PXR transfected in human HepG2 cells assessed as reduction in rifaximin-induced receptor transactivation after 18 hrs by luciferase reporter assay | B | 4.84 | pIC50 | 14600 | nM | IC50 | Eur J Med Chem (2015) 103: 551-562 [PMID:26408814] |
Progesterone receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0] | ||||||||
ChEMBL | DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) | B | 6.21 | pKi | 611 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) | B | 5.33 | pIC50 | 4682 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Sarcoplasmic/endoplasmic reticulum calcium ATP-ase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4693] [UniProtKB: P04191] | ||||||||
ChEMBL | Inhibition of rabbit microsomes SERCA1a by enzyme-coupled method | B | 4.85 | pIC50 | 14000 | nM | IC50 | J Med Chem (2020) 63: 1937-1963 [PMID:32030976] |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 5.86 | pKi | 1369 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 5.32 | pIC50 | 4790 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 5.7 | pKi | 1998 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 5.5 | pIC50 | 3140 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 4.57 | pKi | 26619 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 4.29 | pIC50 | 50819 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 5.22 | pKi | 5986 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 4.89 | pIC50 | 12892 | nM | IC50 | DrugMatrix in vitro pharmacology data |
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 5.18 | pKi | 6637 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 4.9 | pIC50 | 12492 | nM | IC50 | DrugMatrix in vitro pharmacology data |
CYP5A1/Thromboxane-A synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557] | ||||||||
ChEMBL | DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2) | B | 5.36 | pIC50 | 4359 | nM | IC50 | DrugMatrix in vitro pharmacology data |
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] | ||||||||
ChEMBL | DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr)) | B | 4.85 | pIC50 | 14233 | nM | IC50 | DrugMatrix in vitro pharmacology data |
UDP-glucose 4-epimerase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5843] [UniProtKB: Q14376] | ||||||||
ChEMBL | Inhibition of human GalE by HPAEC assay | B | 4.12 | pIC50 | 75000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5744-5747 [PMID:16962325] |
V1A receptor/Vasopressin V1a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288] | ||||||||
ChEMBL | DRUGMATRIX: Vasopressin V1A radioligand binding (ligand: [125I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr) | B | 4.98 | pKi | 10401 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Vasopressin V1A radioligand binding (ligand: [125I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr) | B | 4.59 | pIC50 | 25925 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Estrogen-related receptor-α in Mouse [GtoPdb: 622] [UniProtKB: O08580] | ||||||||
GtoPdb | - | - | 5.3 | pIC50 | - | - | - | Genes Dev (2001) 15: 833-8 [PMID:11297507] |
Estrogen-related receptor-β in Human [GtoPdb: 623] [UniProtKB: O95718] | ||||||||
GtoPdb | - | - | 5.3 | pIC50 | - | - | - | Genes Dev (2001) 15: 833-8 [PMID:11297507] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]