tamsulosin [Ligand Id: 488] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL836 (HGP-0412, HIP-1402, HIP1402, Tamsulon, Tamsulosin, Tamsulosina, Tamsulosine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
| ChEMBL | In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate | F | 9.54 | pKd | 0.29 | nM | Kd | J Med Chem (1997) 40: 3141-3143 [PMID:9379432] |
| ChEMBL | In vitro antagonistic activity against alpha-1A receptor in dog prostate. | F | 9.54 | pKd | 0.29 | nM | Kd | J Med Chem (2001) 44: 1971-1985 [PMID:11384242] |
| ChEMBL | Binding affinity was tested on human Alpha-1A adrenergic receptor | B | 8.4 | pKi | 3.98 | nM | Ki | J Med Chem (1997) 40: 1293-1315 [PMID:9135028] |
| ChEMBL | Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active | B | 9.7 | pKi | 0.2 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 657-664 [PMID:15664832] |
| ChEMBL | Binding affinity was tested on human Alpha-1A adrenergic receptor | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (1997) 40: 1293-1315 [PMID:9135028] |
| ChEMBL | Binding affinity was tested on human Alpha-1A adrenergic receptor | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (1997) 40: 1293-1315 [PMID:9135028] |
| ChEMBL | Displacement of [125I]HEAT from human recombinant adrenergic alpha1A receptor | B | 9.72 | pKi | 0.19 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 640-644 [PMID:18055202] |
| ChEMBL | Binding affinity to human cloned adrenergic alpha-1a receptor | B | 9.72 | pKi | 0.19 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 3930-3934 [PMID:17517507] |
| ChEMBL | Binding affinity to human cloned adrenergic alpha-1A receptor | B | 9.72 | pKi | 0.19 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 3292-3297 [PMID:17452102] |
| ChEMBL | Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand | B | 9.89 | pKi | 0.13 | nM | Ki | J Med Chem (2000) 43: 2183-2195 [PMID:10841797] |
| ChEMBL | Binding affinity towards cloned human alpha-1A adrenergic receptor was determined using [125]-HEAT as radioligand | B | 9.89 | pKi | 0.13 | nM | Ki | J Med Chem (2000) 43: 2183-2195 [PMID:10841797] |
| ChEMBL | Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells | B | 10.3 | pKi | 0.05 | nM | Ki | Eur J Med Chem (2010) 45: 5800-5807 [PMID:20934789] |
| ChEMBL | Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand | B | 10.54 | pKi | 0.03 | nM | Ki | J Med Chem (1997) 40: 3141-3143 [PMID:9379432] |
| GtoPdb | - | - | 10.7 | pKi | - | - | - |
Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248]; Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]; FEBS Lett (1998) 422: 279-83 [PMID:9490024]; Br J Pharmacol (1999) 127: 252-8 [PMID:10369480]; Eur J Pharmacol (1999) 370: 337-43 [PMID:10334511]; J Pharmacol Exp Ther (1995) 272: 134-42 [PMID:7815325]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]; J Pharmacol Exp Ther (2019) 371: 106-112 [PMID:31285236] |
| ChEMBL | Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay | F | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (2016) 59: 9489-9502 [PMID:27709945] |
| ChEMBL | Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay | F | 9.49 | pIC50 | 0.32 | nM | IC50 | Eur J Med Chem (2020) 205: 112616-112616 [PMID:32949920] |
| ChEMBL | Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay | B | 10.15 | pEC50 | 0.07 | nM | EC50 | Bioorg Med Chem (2016) 24: 5582-5591 [PMID:27658792] |
| Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130] | ||||||||
| ChEMBL | In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor | B | 9.9 | pKi | 0.13 | nM | Ki | J Med Chem (1997) 40: 2674-2687 [PMID:9276013] |
| Alpha-1a adrenergic receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3637] [UniProtKB: O02824] | ||||||||
| ChEMBL | Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay | F | 9.8 | pKd | 0.16 | nM | Kd | J Med Chem (1997) 40: 2674-2687 [PMID:9276013] |
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
| ChEMBL | In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens | F | 9.47 | pKd | 0.34 | nM | Kd | J Med Chem (1997) 40: 3141-3143 [PMID:9379432] |
| ChEMBL | In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens | F | 9.47 | pKd | 0.34 | nM | Kd | J Med Chem (2001) 44: 1971-1985 [PMID:11384242] |
| ChEMBL | Displacement of [3H]prazosin from rat salivary gland adrenergic alpha 1A receptor after 45 mins by liquid scintillation counter | B | 9.89 | pKi | 0.13 | nM | Ki | Eur J Med Chem (2011) 46: 3000-3012 [PMID:21549456] |
| ChEMBL | In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A | B | 10.52 | pKi | 0.03 | nM | Ki | J Med Chem (2000) 43: 1586-1603 [PMID:10780916] |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| ChEMBL | Binding affinity was tested on human Alpha-1B adrenergic receptor | B | 7 | pKi | 100 | nM | Ki | J Med Chem (1997) 40: 1293-1315 [PMID:9135028] |
| ChEMBL | Binding affinity to human cloned adrenergic alpha-1b receptor | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 3930-3934 [PMID:17517507] |
| ChEMBL | Binding affinity to human cloned adrenergic alpha-1B receptor | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 3292-3297 [PMID:17452102] |
| ChEMBL | Displacement of [125I]HEAT from human recombinant adrenergic Alpha-1B receptor | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 640-644 [PMID:18055202] |
| ChEMBL | Binding affinity towards cloned human alpha-1B adrenergic receptor was determined using [125]-HEAT as radioligand | B | 8.72 | pKi | 1.92 | nM | Ki | J Med Chem (2000) 43: 2183-2195 [PMID:10841797] |
| ChEMBL | Binding affinity was tested on human Alpha-1B adrenergic receptor | B | 8.9 | pKi | 1.26 | nM | Ki | J Med Chem (1997) 40: 1293-1315 [PMID:9135028] |
| ChEMBL | Binding affinity was tested on human Alpha-1B adrenergic receptor | B | 8.9 | pKi | 1.26 | nM | Ki | J Med Chem (1997) 40: 1293-1315 [PMID:9135028] |
| ChEMBL | Displacement of [3H]prazosin from human Alpha-1B adrenoceptor expressed in CHO cells | B | 9.2 | pKi | 0.63 | nM | Ki | Eur J Med Chem (2010) 45: 5800-5807 [PMID:20934789] |
| ChEMBL | Binding affinity against human adrenergic receptor subtype Alpha-1B adrenergic receptor using [3H]prazosin as radioligand | B | 9.21 | pKi | 0.61 | nM | Ki | J Med Chem (1997) 40: 3141-3143 [PMID:9379432] |
| GtoPdb | - | - | 9.7 | pKi | - | - | - |
Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248]; Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]; Br J Pharmacol (1999) 127: 252-8 [PMID:10369480]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| ChEMBL | Antagonist activity at human alpha1B receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay | F | 8.38 | pIC50 | 4.2 | nM | IC50 | Eur J Med Chem (2020) 205: 112616-112616 [PMID:32949920] |
| Alpha-1b adrenergic receptor in Hamster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3122] [UniProtKB: P18841] | ||||||||
| ChEMBL | In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1b expressed in LTK cell | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2000) 43: 1586-1603 [PMID:10780916] |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823] | ||||||||
| ChEMBL | In vitro antagonism against Alpha-1B adrenergic receptor using phenylephrine (PE) challenge in rat spleen | F | 9.69 | pKd | 0.2 | nM | Kd | J Med Chem (1997) 40: 3141-3143 [PMID:9379432] |
| ChEMBL | In vitro antagonistic activity against alpha-1B receptor in rat spleen. | F | 9.69 | pKd | 0.2 | nM | Kd | J Med Chem (2001) 44: 1971-1985 [PMID:11384242] |
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
| ChEMBL | Binding affinity was tested on human Alpha-1D adrenergic receptor | B | 8.1 | pKi | 7.94 | nM | Ki | J Med Chem (1997) 40: 1293-1315 [PMID:9135028] |
| ChEMBL | Displacement of [125I]HEAT from human recombinant adrenergic alpha1C receptor | B | 9.7 | pKi | 0.2 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 640-644 [PMID:18055202] |
| ChEMBL | Binding affinity to human cloned adrenergic alpha-1d receptor | B | 9.7 | pKi | 0.2 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 3930-3934 [PMID:17517507] |
| ChEMBL | Binding affinity to human cloned adrenergic Alpha-1D receptor | B | 9.7 | pKi | 0.2 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 3292-3297 [PMID:17452102] |
| ChEMBL | Displacement of [125I] HEAT from human alpha1D adrenergic receptor expressed in Chlorocebus aethiops COS1 cell membranes incubated for 60 mins by liquid scintillation counting analysis | B | 9.74 | pKi | 0.18 | nM | Ki | J Med Chem (2016) 59: 2989-3002 [PMID:26954848] |
| ChEMBL | Binding affinity towards cloned human alpha-1D adrenergic receptor was determined using [125]-HEAT as radioligand | B | 9.74 | pKi | 0.18 | nM | Ki | J Med Chem (2000) 43: 2183-2195 [PMID:10841797] |
| ChEMBL | Binding affinity was tested on human Alpha-1D adrenergic receptor | B | 9.8 | pKi | 0.16 | nM | Ki | J Med Chem (1997) 40: 1293-1315 [PMID:9135028] |
| ChEMBL | Binding affinity was tested on human Alpha-1D adrenergic receptor | B | 9.8 | pKi | 0.16 | nM | Ki | J Med Chem (1997) 40: 1293-1315 [PMID:9135028] |
| ChEMBL | Displacement of [3H]prazosin from human Alpha-1D adrenoceptor expressed in CHO cells | B | 10 | pKi | 0.1 | nM | Ki | Eur J Med Chem (2010) 45: 5800-5807 [PMID:20934789] |
| GtoPdb | - | - | 10.2 | pKi | - | - | - |
Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248]; Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]; Br J Pharmacol (1999) 127: 252-8 [PMID:10369480]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| ChEMBL | Binding affinity against human adrenergic receptor subtype Alpha-1D adrenergic receptor using [3H]prazosin as radioligand | B | 10.24 | pKi | 0.06 | nM | Ki | J Med Chem (1997) 40: 3141-3143 [PMID:9379432] |
| ChEMBL | Antagonist activity at human full-length N-terminal SNAP-tagged alpha1D adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay | F | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2016) 59: 9489-9502 [PMID:27709945] |
| ChEMBL | Antagonist activity at human alpha1D receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay | F | 9.82 | pIC50 | 0.15 | nM | IC50 | Eur J Med Chem (2020) 205: 112616-112616 [PMID:32949920] |
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944] | ||||||||
| ChEMBL | In vitro antagonism against Alpha-1D adrenergic receptor using phenylephrine (PE) challenge in rat aorta | F | 10.6 | pKd | 0.03 | nM | Kd | J Med Chem (1997) 40: 3141-3143 [PMID:9379432] |
| ChEMBL | In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1d expressed in LTK cell | B | 10.15 | pKi | 0.07 | nM | Ki | J Med Chem (2000) 43: 1586-1603 [PMID:10780916] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | Binding affinity towards recombinant human alpha-2A adrenergic receptor was determined using [3H]MK-912 as radioligand | B | 7.2 | pKi | 63 | nM | Ki | J Med Chem (2000) 43: 2183-2195 [PMID:10841797] |
| ChEMBL | Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand | B | 7.87 | pKi | 13.4 | nM | Ki | J Med Chem (1997) 40: 3141-3143 [PMID:9379432] |
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328] | ||||||||
| ChEMBL | Binding affinity towards rat alpha-2B adrenergic receptor was determined using [3H]yohimbine as radioligand | B | 7.1 | pKi | 80 | nM | Ki | J Med Chem (2000) 43: 2183-2195 [PMID:10841797] |
| ChEMBL | Binding affinity against rat Alpha-2B adrenergic receptor using [3H]rauwolscine as radioligand | B | 8.17 | pKi | 6.8 | nM | Ki | J Med Chem (1997) 40: 3141-3143 [PMID:9379432] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| ChEMBL | Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligand | B | 8.1 | pKi | 7.9 | nM | Ki | J Med Chem (1997) 40: 3141-3143 [PMID:9379432] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Binding affinity towards recombinant human Dopamine receptor D2S was determined using [3H]spiperone as radioligand | B | 7.11 | pKi | 78 | nM | Ki | J Med Chem (2000) 43: 2183-2195 [PMID:10841797] |
| ChEMBL | Binding affinity towards recombinant human Dopamine receptor D2L was determined using [3H]spiperone as radioligand | B | 7.89 | pKi | 13 | nM | Ki | J Med Chem (2000) 43: 2183-2195 [PMID:10841797] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Binding affinity towards recombinant human Dopamine receptor D3 was determined using [3H]spiperone as radioligand | B | 9.55 | pKi | 0.28 | nM | Ki | J Med Chem (2000) 43: 2183-2195 [PMID:10841797] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Binding affinity towards recombinant human Compound at 1 uM was tested for the inhibition of radioligand [3H]8-OH-DPAT binding to recombinant human 5-hydroxytryptamine 1A receptor was determined using [3H]8-OH-DPAT as radioligand | B | 9.1 | pKi | 0.79 | nM | Ki | J Med Chem (2000) 43: 2183-2195 [PMID:10841797] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Binding affinity towards recombinant human 5-hydroxytryptamine 7 receptor was determined using [3H]LSD as radioligand | B | 7.08 | pKi | 84 | nM | Ki | J Med Chem (2000) 43: 2183-2195 [PMID:10841797] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
