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] There should be some charts here, you may need to enable JavaScript!
H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021] There should be some charts here, you may need to enable JavaScript!
histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] There should be some charts here, you may need to enable JavaScript!
NK2 receptor/Neurokinin 2 receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452] There should be some charts here, you may need to enable JavaScript!

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]
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
ChEMBL	Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate	B	6.28	pIC50	528.4	nM	IC50	HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators
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 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]