flavanone [Ligand Id: 408] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL274318
  • A1 receptor/Adenosine receptor A1 in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • A3 receptor/Adenosine receptor A3 in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • Monoamine oxidase B/Amine oxidase [flavin-containing] B in Human [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A1 receptor/Adenosine receptor A1 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 4.49 pKi 32000 nM Ki J Med Chem (1996) 39: 2293-2301 [PMID:8691424]
GtoPdb - - 4.5 pKi - - - J Med Chem (1996) 39: 2293-301 [PMID:8691424]
A3 receptor/Adenosine receptor A3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
GtoPdb - - 4.3 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 4.3 pKi 50100 nM Ki J Med Chem (1996) 39: 2293-2301 [PMID:8691424]
Monoamine oxidase B/Amine oxidase [flavin-containing] B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338]
ChEMBL Inhibition of human recombinant MAOB expressed in BTI-TN-5B1-4 cells by para-tyramine oxidation assay B 5.54 pIC50 2870 nM IC50 Bioorg Med Chem (2010) 18: 1273-1279 [PMID:20045650]
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 4.7 pIC50 20000 nM IC50 Bioorg Med Chem Lett (2009) 19: 4706-4710 [PMID:19592245]
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 4.26 pIC50 54954.09 nM IC50 J Med Chem (2005) 48: 5666-5674 [PMID:16134935]
CYP19A1/Aromatase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511]
ChEMBL In vitro inhibition of [1,2,6,7-3H]-androstenedione binding to human placental microsome cytochrome P450 19A1 B 4.55 pIC50 28500 nM IC50 Bioorg Med Chem Lett (2002) 12: 1059-1061 [PMID:11909717]
ChEMBL Inhibition of human aromatase in placental microsomes B 4.55 pIC50 28000 nM IC50 Bioorg Med Chem (2008) 16: 1474-1480 [PMID:18042388]
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 4.86 pIC50 13803.84 nM IC50 Eur J Med Chem (2017) 137: 365-438 [PMID:28622580]
ChEMBL Inhibition of aromatase (unknown origin) B 5.1 pIC50 8000 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 data shown on this page come from version 36:

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]