ChEMBL ligand: CHEMBL1201199 (ABBOTT-43818 FREE BASE, CKD-841, Leuporelin, (-)-leuprolide, Leuprolide, Leuprorelin, Leuprorelina, Leuproreline, Leuprorelin slow release, NSC-377526, TAP-144 FREE BASE)
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!
MRGPRX2/Mas-related G-protein coupled receptor member X2 in Human [ChEMBL: CHEMBL5849] [GtoPdb: 157] [UniProtKB: Q96LB1] 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]
GtoPdb	-	-	9.1	pKi	0.79	nM	Ki	Endocrinology (2007) 148: 857-67 [PMID:17095587]
ChEMBL	Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor	B	9.1	pIC50	0.8	nM	IC50	J Med Chem (2006) 49: 3809-3825 [PMID:16789738]
ChEMBL	The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor	B	9.52	pIC50	0.3	nM	IC50	J Med Chem (1998) 41: 4190-4195 [PMID:9784092]
ChEMBL	Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells	B	9.52	pIC50	0.3	nM	IC50	J Med Chem (2006) 49: 3809-3825 [PMID:16789738]
ChEMBL	Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis	B	9.54	pIC50	0.29	nM	IC50	Medchemcomm (2015) 6: 1656-1665
GnRH1 receptor/Gonadotropin-releasing hormone receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3066] [GtoPdb: 256] [UniProtKB: P30969]
ChEMBL	The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary	B	9.1	pIC50	0.8	nM	IC50	J Med Chem (1998) 41: 4190-4195 [PMID:9784092]
GtoPdb	-	-	9.1	pIC50	-	-	-	Endocrinology (1994) 135: 315-20 [PMID:8013367]
ChEMBL	The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary	B	9.3	pIC50	0.5	nM	IC50	J Med Chem (1998) 41: 4190-4195 [PMID:9784092]
ChEMBL	Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor	B	9.3	pIC50	0.5	nM	IC50	J Med Chem (2006) 49: 3809-3825 [PMID:16789738]
MRGPRX2/Mas-related G-protein coupled receptor member X2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5849] [GtoPdb: 157] [UniProtKB: Q96LB1]
ChEMBL	Agonist activity at N-terminal Flag-tagged human MRGPRX2 receptor expressed in tetracycline-induced FLP-IN/T-REX 293 cells assessed as increase in intracellular calcium release by FLIPR assay	F	4.5	pEC50	>31622.78	nM	EC50	Nat Chem Biol (2017) 13: 529-536 [PMID:28288109]
ChEMBL	Agonist activity at MRGPRX2 (unknown origin) expressed in HTLA cells assessed as induction of beta-arrestin 2 recruitment incubated for 18 to 24 hrs by PRESTO-Tango assay	F	4.5	pEC50	>31622.78	nM	EC50	Nat Chem Biol (2017) 13: 529-536 [PMID:28288109]

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]