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ChEMBL ligand: CHEMBL474991 (WAY-207024) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]