galangin [Ligand Id: 410] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL309490 (NSC-407229)
  • 3-oxoacyl-acyl-carrier protein reductase in Plasmodium falciparum [ChEMBL: CHEMBL4513] [UniProtKB: Q965D6]
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  • acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
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  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • butyrylcholinesterase/Butyrylcholinesterase in Human [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276]
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  • carbonic anhydrase 1/Carbonic anhydrase I in Human [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
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  • carbonic anhydrase 2/Carbonic anhydrase II in Human [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
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  • carbonic anhydrase 4/Carbonic anhydrase IV in Human [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748]
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  • carbonic anhydrase 7/Carbonic anhydrase VII in Human [ChEMBL: CHEMBL2326] [GtoPdb: 2749] [UniProtKB: P43166]
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  • carbonic anhydrase 12/Carbonic anhydrase XII in Human [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570]
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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • xanthine dehydrogenase/Xanthine dehydrogenase in Human [ChEMBL: CHEMBL1929] [GtoPdb: 2646] [UniProtKB: P47989]
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  • TRPC5 in Human [GtoPdb: 490] [UniProtKB: Q9UL62]
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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]
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]
TRPC5 in Human [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 data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]