WAY-207024 [Ligand Id: 5582] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL474991 (WAY-207024)
  • GnRH1 receptor/Gonadotropin-releasing hormone receptor in Human [ChEMBL: CHEMBL1855] [GtoPdb: 256] [UniProtKB: P30968]
  • GnRH1 receptor/Gonadotropin-releasing hormone receptor in Rat [ChEMBL: CHEMBL3066] [GtoPdb: 256] [UniProtKB: P30969]
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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
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  • NK2 receptor/Neurokinin 2 receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GnRH1 receptor/Gonadotropin-releasing hormone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1855] [GtoPdb: 256] [UniProtKB: P30968]
ChEMBL Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction F 7.55 pIC50 28 nM IC50 J Med Chem (2009) 52: 2148-2152 [PMID:19271735]
ChEMBL Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay F 7.55 pIC50 28 nM IC50 Bioorg Med Chem Lett (2010) 20: 2512-2515 [PMID:20236823]
GtoPdb - - 7.92 pIC50 12 nM IC50 J Med Chem (2009) 52: 2148-52 [PMID:19271735]
ChEMBL Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptor B 7.92 pIC50 12 nM IC50 J Med Chem (2009) 52: 2148-2152 [PMID:19271735]
ChEMBL Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting B 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2010) 20: 2512-2515 [PMID:20236823]
GnRH1 receptor/Gonadotropin-releasing hormone receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3066] [GtoPdb: 256] [UniProtKB: P30969]
ChEMBL Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA F 6.44 pIC50 360 nM IC50 Bioorg Med Chem Lett (2010) 20: 2512-2515 [PMID:20236823]
ChEMBL Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells F 6.49 pIC50 320 nM IC50 J Med Chem (2009) 52: 2148-2152 [PMID:19271735]
ChEMBL Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting B 7.14 pIC50 72 nM IC50 Bioorg Med Chem Lett (2010) 20: 2512-2515 [PMID:20236823]
ChEMBL Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor B 7.15 pIC50 71 nM IC50 J Med Chem (2009) 52: 2148-2152 [PMID:19271735]
GtoPdb - - 7.15 pIC50 71 nM IC50 J Med Chem (2009) 52: 2148-52 [PMID:19271735]
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
ChEMBL Inhibition of human histamine H2 receptor B 6.07 pKi 850 nM Ki J Med Chem (2009) 52: 2148-2152 [PMID:19271735]
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
ChEMBL Inhibition of human neurokinin NK2 receptor B 6.48 pKi 330 nM Ki J Med Chem (2009) 52: 2148-2152 [PMID:19271735]

ChEMBL data shown on this page come from version 33:

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]