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 (Yt 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] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| ChEMBL | Binding affinity to PPARgamma (unknown origin) assessed as inhibition constant by Lanthascreen TR-FRET assay relative to control | B | 5.25 | pKi | 5600 | nM | Ki | Bioorg Med Chem (2022) 54: 116564-116564 [PMID:34922307] |
| 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] |
| Protein disulfide-isomerase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5422] [UniProtKB: P07237] | ||||||||
| ChEMBL | Binding affinity to recombinant His-tagged full length human PDI-b' x domain substrate binding pocket expressed in Escherichia coli BL21 (DE3) cells assessed as inhibition constant at 100 uM incubated for 10 mins by tryptophan fluorescence based assay | B | 5.23 | pKi | 5900 | nM | Ki | J Nat Prod (2022) 85: 1332-1339 [PMID:35471830] |
| 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 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]
