flavone [Ligand Id: 409] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL275638 (2-phenyl-1,4-benzopyrone, 2-phenyl-.gamma.-benzopyrone, Asmacoril, Chromocor, Cromaril, Cromarile, Flavone, NSC-19028)
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • A2A receptor in Human [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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  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
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  • ABCG2/ATP-binding cassette sub-family G member 2 in Human [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
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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 9/Carbonic anhydrase IX in Human [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790]
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  • carbonic anhydrase 12/Carbonic anhydrase XII in Human [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570]
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  • Dihydroorotate dehydrogenase in Plasmodium falciparum [ChEMBL: CHEMBL3486] [UniProtKB: Q54A96]
  • Dihydroorotate dehydrogenase in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL5621] [UniProtKB: P28272]
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  • dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Human [ChEMBL: CHEMBL284] [GtoPdb: 1612] [UniProtKB: P27487]
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  • protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
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  • poly(ADP-ribose) polymerase 1/Poly [ADP-ribose] polymerase-1 in Human [ChEMBL: CHEMBL3105] [GtoPdb: 2771] [UniProtKB: P09874]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 5.48 pKi 3280 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 5.48 pKi 3280 nM Ki J Med Chem (1996) 39: 781-788 [PMID:8576921]
GtoPdb - - 5.5 pKi - - - J Med Chem (1996) 39: 2293-301 [PMID:8691424]
A2A receptor in Human [GtoPdb: 19] [UniProtKB: P29274]
GtoPdb - - 5.5 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 5.46 pKi 3450 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]
ChEMBL Binding affinity against human adenosine A3 receptor in HEK293 cells using [125I]AB-MECA 21680 radioligand. B 4.77 pKi 16900 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 4.77 pKi 16900 nM Ki J Med Chem (1996) 39: 781-788 [PMID:8576921]
GtoPdb - - 4.8 pKi - - - J Med Chem (1996) 39: 2293-301 [PMID:8691424]
Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
ChEMBL Antagonist activity at androgen receptor in human MDA-kb2 cells assessed as inhibition of DHT-induced luciferase activity by luciferase reporter gene assay F 5.23 pIC50 5900 nM IC50 Bioorg Med Chem Lett (2009) 19: 4706-4710 [PMID:19592245]
ChEMBL Antagonist activity at androgen receptor in human MDA-kb2 cells assessed as inhibition of DHT-induced luciferase activity by luciferase reporter gene assay F 5.23 pIC50 5900 nM IC50 Bioorg Med Chem Lett (2009) 19: 4706-4710 [PMID:19592245]
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 4.11 pIC50 77624.71 nM IC50 J Med Chem (2005) 48: 5666-5674 [PMID:16134935]
ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
ChEMBL Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining B 4.59 pIC50 26000 nM IC50 Bioorg Med Chem (2011) 19: 2090-2102 [PMID:21354800]
ChEMBL Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining B 4.77 pIC50 17000 nM IC50 Bioorg Med Chem (2011) 19: 2090-2102 [PMID:21354800]
carbonic anhydrase 1/Carbonic anhydrase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
ChEMBL Inhibition of cytosolic human carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay B 5.72 pKi 1890 nM Ki Bioorg Med Chem Lett (2012) 22: 3063-3066 [PMID:22487176]
ChEMBL Inhibition of cytosolic human carbonic anhydrase 1 preincubated for 12 hrs by stopped flow CO2 hydration assay B 5.73 pKi 1880 nM Ki Bioorg Med Chem Lett (2012) 22: 3063-3066 [PMID:22487176]
carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
ChEMBL Inhibition of cytosolic human carbonic anhydrase 2 preincubated for 12 hrs by stopped flow CO2 hydration assay B 5.06 pKi 8800 nM Ki Bioorg Med Chem Lett (2012) 22: 3063-3066 [PMID:22487176]
ChEMBL Inhibition of cytosolic human carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay B 5.06 pKi 8710 nM Ki Bioorg Med Chem Lett (2012) 22: 3063-3066 [PMID:22487176]
carbonic anhydrase 9/Carbonic anhydrase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790]
ChEMBL Inhibition of transmembrane tumor-associated human carbonic anhydrase 9 preincubated for 12 hrs by stopped flow CO2 hydration assay B 5.37 pKi 4220 nM Ki Bioorg Med Chem Lett (2012) 22: 3063-3066 [PMID:22487176]
ChEMBL Inhibition of transmembrane tumor-associated human carbonic anhydrase 9 preincubated for 15 mins by stopped flow CO2 hydration assay B 5.38 pKi 4130 nM Ki Bioorg Med Chem Lett (2012) 22: 3063-3066 [PMID:22487176]
carbonic anhydrase 12/Carbonic anhydrase XII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570]
ChEMBL Inhibition of transmembrane tumor-associated human carbonic anhydrase 12 preincubated for 12 hrs by stopped flow CO2 hydration assay B 5.13 pKi 7330 nM Ki Bioorg Med Chem Lett (2012) 22: 3063-3066 [PMID:22487176]
ChEMBL Inhibition of transmembrane tumor-associated human carbonic anhydrase 12 preincubated for 15 mins by stopped flow CO2 hydration assay B 5.14 pKi 7220 nM Ki Bioorg Med Chem Lett (2012) 22: 3063-3066 [PMID:22487176]
CYP19A1/Cytochrome P450 19A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511]
ChEMBL Inhibition of human aromatase using ASD as substrate pre-incubated for 5 mins followed by substrate addition and measured after 16 hrs by UV/vis-spectrophotometry B 4.32 pIC50 47973.34 nM IC50 Eur J Med Chem (2017) 137: 365-438 [PMID:28622580]
ChEMBL Inhibition of aromatase (unknown origin) B 5 pIC50 10000 nM IC50 Bioorg Med Chem (2014) 22: 126-134 [PMID:24345481]
ChEMBL Inhibition of aromatase (unknown origin) B 5.1 pIC50 8000 nM IC50 Eur J Med Chem (2015) 102: 375-386 [PMID:26301554]
ChEMBL Inhibition of human placental microsome CYP19 B 8.1 pIC50 8 nM IC50 Bioorg Med Chem Lett (2010) 20: 3050-3064 [PMID:20413308]
CYP1B1/Cytochrome P450 1B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4878] [GtoPdb: 1320] [UniProtKB: Q16678]
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 6.22 pIC50 600 nM IC50 Eur J Med Chem (2017) 135: 296-306 [PMID:28458135]
Dihydroorotate dehydrogenase in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3486] [UniProtKB: Q54A96]
ChEMBL Inhibition of Plasmodium falciparum DHOD B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2009) 19: 972-975 [PMID:19097788]
Dihydroorotate dehydrogenase in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5621] [UniProtKB: P28272]
ChEMBL Inhibition of Saccharomyces cerevisiae DHOD B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2009) 19: 972-975 [PMID:19097788]
dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL284] [GtoPdb: 1612] [UniProtKB: P27487]
ChEMBL Inhibition of DPP4 (unknown origin) using Gly-Pro-AMC as substrate preincubated for 4 secs followed by substrate addition and measured after 30 mins by luminescence assay B 6.77 pIC50 170 nM IC50 Eur J Med Chem (2018) 151: 145-157 [PMID:29609120]
protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
ChEMBL Inhibition of DNA dependent protein kinase isolated from HeLa cells B 5 pIC50 >10000 nM IC50 J Med Chem (2005) 48: 569-585 [PMID:15658870]
GABAA receptor π subunit/GABAA receptor δ subunit/GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABAA receptor α4 subunit/GABAA receptor ε subunit/GABAA receptor α6 subunit/GABAA receptor γ1 subunit/GABAA receptor γ3 subunit/GABAA receptor θ subunit/GABA-A receptor; anion channel in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093872] [GtoPdb: 419, 416, 404, 410, 414, 412, 408, 406, 405, 411, 407, 417, 409, 413, 415, 418] [UniProtKB: O00591, O14764, P14867, P18505, P18507, P28472, P31644, P34903, P47869, P47870, P48169, P78334, Q16445, Q8N1C3, Q99928, Q9UN88]
ChEMBL Binding affinity towards benzodiazepine site in GABAA receptor B 6 pKi 1000 nM Ki J Med Chem (2001) 44: 1883-1891 [PMID:11384234]
ChEMBL Inhibition of binding to GABA-A Benzodiazepine receptor B 7.77 pKi 17 nM Ki J Med Chem (1999) 42: 3743-3778 [PMID:10508425]
GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14]
ChEMBL In vitro affinity against Benzodiazepine receptor binding to rat cortical membranes (using [3H]- flumazenil as radioligand). B 5.38 pKi 4200 nM Ki J Med Chem (1999) 42: 4343-4350 [PMID:10543878]
ChEMBL Ability to inhibit [3H]-Ro- 15-1788 binding to Gamma-aminobutyric acid A receptor alpha in vitro in rat cortical membranes B 5.38 pKi 4200 nM Ki J Med Chem (2002) 45: 4188-4201 [PMID:12213060]
ChEMBL Displacement of [3H]flunitrazepine binding from GABA-A central benzodiazepine receptor of rat cerebral cortical membrane B 6 pKi 1000 nM Ki Bioorg Med Chem Lett (1997) 7: 2003-2008
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 4.47 pKd 33884.42 nM Kd Eur J Med Chem (2011) 46: 4078-4088 [PMID:21723648]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 F 4.22 pIC50 60800 nM IC50 J Med Chem (2006) 49: 3345-3353 [PMID:16722653]
ChEMBL Antimalarial activity against Plasmodium falciparum DD2 expressing Saccharomyces cerevisiae DHOD by [3H]hypoxanthine uptake F 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2009) 19: 972-975 [PMID:19097788]
ChEMBL Antimalarial activity against Plasmodium falciparum DD2 by [3H]hypoxanthine uptake F 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (2009) 19: 972-975 [PMID:19097788]
poly(ADP-ribose) polymerase 1/Poly [ADP-ribose] polymerase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3105] [GtoPdb: 2771] [UniProtKB: P09874]
ChEMBL Inhibition of human recombinant ARTD1 by fluorescence assay B 5.85 pIC50 1400 nM IC50 J Med Chem (2013) 56: 3507-3517 [PMID:23574272]
ChEMBL Inhibition of human recombinant ARTD1 by fluorescence assay B 5.86 pIC50 1380.38 nM IC50 J Med Chem (2013) 56: 3507-3517 [PMID:23574272]
tankyrase/Tankyrase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6164] [GtoPdb: 3108] [UniProtKB: O95271]
ChEMBL Inhibition of human TNKS1 (1030 to 1317) using NAD+ as substrate by fluorescence assay B 6.48 pIC50 330 nM IC50 J Med Chem (2013) 56: 7880-7889 [PMID:24116873]
ChEMBL Inhibition of human 6XHis-tagged TNKS1 SAM-ART domain (1030 to 1317 amino acid residues) by fluorescence assay B 6.49 pIC50 323.59 nM IC50 J Med Chem (2013) 56: 3507-3517 [PMID:23574272]
ChEMBL Inhibition of human TNKS1 (1030 to 1317) using NAD+ as substrate by fluorescence assay B 6.49 pIC50 323.59 nM IC50 J Med Chem (2013) 56: 7880-7889 [PMID:24116873]
ChEMBL Inhibition of human 6XHis-tagged TNKS1 SAM-ART domain (1030 to 1317 amino acid residues) by fluorescence assay B 6.49 pIC50 320 nM IC50 J Med Chem (2013) 56: 3507-3517 [PMID:23574272]
tankyrase 2/Tankyrase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6154] [GtoPdb: 3109] [UniProtKB: Q9H2K2]
ChEMBL Inhibition of human 6XHis-tagged TNKS2 ART domain (946 to 1161 amino acid residues) expressed in Escherichia coli Rosetta2 (DE3) by fluorescence assay B 6.83 pIC50 147.91 nM IC50 J Med Chem (2013) 56: 3507-3517 [PMID:23574272]
ChEMBL Inhibition of human 6XHis-tagged TNKS2 ART domain (946 to 1161 amino acid residues) expressed in Escherichia coli Rosetta2 (DE3) by fluorescence assay B 6.85 pIC50 140 nM IC50 J Med Chem (2013) 56: 3507-3517 [PMID:23574272]

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]