galangin [Ligand Id: 410] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL309490 (NSC-407229) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 3-oxoacyl-acyl-carrier protein reductase in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4513] [UniProtKB: Q965D6] | ||||||||
| ChEMBL | Inhibition of FabG | B | 4 | pIC50 | 100000 | nM | IC50 | J Med Chem (2006) 49: 3345-3353 [PMID:16722653] |
| acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303] | ||||||||
| ChEMBL | Inhibition of human recombinant AChE by Ellman's method | B | 4.07 | pKi | 85600 | nM | Ki | Eur J Med Chem (2010) 45: 186-192 [PMID:19879672] |
| ChEMBL | Inhibition of AChE (unknown origin) | B | 7.92 | pIC50 | 12 | nM | IC50 | Med Chem Res (2013) 22: 3061-3075 |
| A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
| ChEMBL | Binding affinity at Adenosine A1 receptor in rat brain membranes by [3H]PIA displacement. | B | 6.06 | pKi | 863 | nM | Ki | J Med Chem (1996) 39: 2293-2301 [PMID:8691424] |
| ChEMBL | Displacement of specific [3H]PIA binding from adenosine A1 receptor in rat brain membranes. | B | 6.06 | pKi | 863 | nM | Ki | J Med Chem (1996) 39: 781-788 [PMID:8576921] |
| GtoPdb | - | - | 6.1 | pKi | - | - | - | J Med Chem (1996) 39: 2293-301 [PMID:8691424] |
| A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
| ChEMBL | Binding affinity for HA-tagged mutant human Adenosine A2A receptor (H250N) using [3H]-CGS-21,680 as radioligand expressed in COS-7 cells | B | 4.48 | pKi | 33000 | nM | Ki | J Med Chem (1997) 40: 2588-2595 [PMID:9258366] |
| ChEMBL | Binding affinity for HA-tagged mutant human Adenosine A2A receptor (V84L), using [3H]CGS-21680 as radioligand expressed in COS-7 cells | B | 4.74 | pKi | 18100 | nM | Ki | J Med Chem (1997) 40: 2588-2595 [PMID:9258366] |
| ChEMBL | Binding affinity for HA-tagged wild type human Adenosine A2A receptor (WT) using [3H]CGS-21680 as radioligand expressed in COS-7 cells | B | 4.78 | pKi | 16700 | nM | Ki | J Med Chem (1997) 40: 2588-2595 [PMID:9258366] |
| GtoPdb | - | - | 6 | pKi | - | - | - | J Med Chem (1996) 39: 2293-301 [PMID:8691424] |
| A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
| ChEMBL | Affinity at Adenosine A2A receptor in rat striatal membranes by [3H]- CGS 21680 displacement. | B | 6.02 | pKi | 966 | nM | Ki | J Med Chem (1996) 39: 781-788 [PMID:8576921] |
| A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
| GtoPdb | - | - | 5.5 | pKi | - | - | - | J Med Chem (1996) 39: 2293-301 [PMID:8691424] |
| ChEMBL | Binding affinity against human adenosine A3 receptor in HEK293 cells using [125I]AB-MECA 21680 radioligand. | B | 5.5 | pKi | 3150 | nM | Ki | J Med Chem (1996) 39: 2293-2301 [PMID:8691424] |
| ChEMBL | Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells | B | 5.5 | pKi | 3150 | nM | Ki | J Med Chem (1996) 39: 781-788 [PMID:8576921] |
| butyrylcholinesterase/Butyrylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276] | ||||||||
| ChEMBL | Inhibition of human plasma BChE by Ellman's method | B | 5.16 | pKi | 6900 | nM | Ki | Eur J Med Chem (2010) 45: 186-192 [PMID:19879672] |
| carbonic anhydrase 1/Carbonic anhydrase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915] | ||||||||
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins at room temperature/6 hrs at 4 deg C by stopped-flow CO2 hydration assay | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2015) 23: 7219-7225 [PMID:26498393] |
| carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918] | ||||||||
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins at room temperature/6 hrs at 4 deg C by stopped-flow CO2 hydration assay | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2015) 23: 7219-7225 [PMID:26498393] |
| carbonic anhydrase 4/Carbonic anhydrase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748] | ||||||||
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 4 preincubated for 15 mins at room temperature/6 hrs at 4 deg C by stopped-flow CO2 hydration assay | B | 6.25 | pKi | 568.3 | nM | Ki | Bioorg Med Chem (2015) 23: 7219-7225 [PMID:26498393] |
| carbonic anhydrase 7/Carbonic anhydrase VII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2326] [GtoPdb: 2749] [UniProtKB: P43166] | ||||||||
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 7 preincubated for 15 mins at room temperature/6 hrs at 4 deg C by stopped-flow CO2 hydration assay | B | 7.61 | pKi | 24.5 | nM | Ki | Bioorg Med Chem (2015) 23: 7219-7225 [PMID:26498393] |
| carbonic anhydrase 12/Carbonic anhydrase XII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570] | ||||||||
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 12 preincubated for 15 mins at room temperature/6 hrs at 4 deg C by stopped-flow CO2 hydration assay | B | 7.38 | pKi | 41.8 | nM | Ki | Bioorg Med Chem (2015) 23: 7219-7225 [PMID:26498393] |
| CYP19A1/Cytochrome P450 19A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511] | ||||||||
| ChEMBL | Inhibition of human aromatase expressed in CHO cells | B | 4 | pKi | 100000 | nM | Ki | Bioorg Med Chem (2008) 16: 8466-8470 [PMID:18778944] |
| CYP1B1/Cytochrome P450 1B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4878] [GtoPdb: 1320] [UniProtKB: Q16678] | ||||||||
| ChEMBL | Inhibition of human CYP1B1 by EROD assay | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem (2010) 18: 6310-6315 [PMID:20696580] |
| ChEMBL | Inhibition of human CYP1B1 expressed in Escherichia coli DH5alpha coexpressing human NADPH P450 reductase using 7-ethoxyresorufin as substrate in presence of NADP+ by spectrofluorometeric analysis | B | 8.52 | pIC50 | 3 | nM | IC50 | Eur J Med Chem (2017) 135: 296-306 [PMID:28458135] |
| Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397] | ||||||||
| ChEMBL | Inhibition of recombinant human MAO-A assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate after 20 mins by fluorometric assay | B | 6.89 | pIC50 | 130 | nM | IC50 | J Nat Prod (2016) 79: 2538-2544 [PMID:27754693] |
| Monoamine oxidase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338] | ||||||||
| ChEMBL | Inhibition of recombinant human MAO-B assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate after 20 mins by fluorometric assay | B | 5.44 | pIC50 | 3650 | nM | IC50 | J Nat Prod (2016) 79: 2538-2544 [PMID:27754693] |
| ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
| ChEMBL | Binding affinity to ABCB1 nucleotide binding domain 2 | B | 5.23 | pKd | 5888.44 | nM | Kd | Eur J Med Chem (2011) 46: 4078-4088 [PMID:21723648] |
| ABCB1/P-glycoprotein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447] | ||||||||
| ChEMBL | Binding affinity to nucleotide-binding domain (NBD2) of P-Glycoprotein | B | 5.23 | pKd | 5900 | nM | Kd | Bioorg Med Chem Lett (2001) 11: 75-77 [PMID:11140738] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 | F | 4.4 | pIC50 | 39400 | nM | IC50 | J Med Chem (2006) 49: 3345-3353 [PMID:16722653] |
| Sarcoplasmic/endoplasmic reticulum calcium ATP-ase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4693] [UniProtKB: P04191] | ||||||||
| ChEMBL | Inhibition of rabbit skeletal muscle microsomes SERCA1a preincubated for 10 mins followed by addition of ATP and measured after 40 mins | B | 5.05 | pIC50 | 9000 | nM | IC50 | J Med Chem (2020) 63: 1937-1963 [PMID:32030976] |
| TRPC5/Short transient receptor potential channel 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1250411] [GtoPdb: 490] [UniProtKB: Q9UL62] | ||||||||
| GtoPdb | Inhibition of lanthanide-evoked calcium entry in HEK 293 cells overexpressing hTRPC5, by patch-clamp recording. | - | 6.35 | pKi | 450 | nM | Ki | Br J Pharmacol (2016) 173: 562-74 [PMID:26565375] |
| ChEMBL | Inhibition of human TRPC5 expressed in HEK293 cells assessed as reduction in gadolinium-induced calcium entry after 30 mins by fluo-4 dye based fluorescence assay | B | 6.35 | pIC50 | 450 | nM | IC50 | J Med Chem (2019) 62: 7589-7602 [PMID:30943030] |
| Tyrosinase in Agaricus bisporus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3318] [UniProtKB: O42713] | ||||||||
| ChEMBL | Inhibition of mushroom tyrosinase | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2009) 17: 6048-6053 [PMID:19615910] |
| fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| ChEMBL | Inhibition of recombinant FLT3 (unknown origin) by TR-FRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1768-1770 [PMID:23411073] |
| xanthine dehydrogenase/Xanthine dehydrogenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1929] [GtoPdb: 2646] [UniProtKB: P47989] | ||||||||
| ChEMBL | Inhibition of xanthine oxidase assessed as decrease in uric acid production by spectrophotometry | B | 5.74 | pIC50 | 1800 | nM | IC50 | J Nat Prod (1998) 61: 71-76 [PMID:9461655] |
ChEMBL data shown on this page come from version 32:
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]
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