ChEMBL ligand: CHEMBL414173
apelin receptor/Apelin receptor in Human [ChEMBL: CHEMBL1628481] [GtoPdb: 36] [UniProtKB: P35414] 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
apelin receptor/Apelin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1628481] [GtoPdb: 36] [UniProtKB: P35414]
ChEMBL	Displacement of [125I] [NIe75,Tyr77]Pyr-apelin-13 from YFP-tagged human APJ receptor expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	B	9.15	pKi	0.7	nM	Ki	J Med Chem (2021) 64: 5345-5364 [PMID:33524256]
GtoPdb	-	-	9.5	pIC50	-	-	-	J Biol Chem (2000) 275: 21061-7 [PMID:10777510]; J Neurochem (2003) 84: 1162-1172 [PMID:12603839]; Biochemistry (2003) 42: 10163-8 [PMID:12939143]
ChEMBL	GPCR PRESTO-Tango dose-response in agonist mode with target: APLNR	F	6.92	pEC50	119.43	nM	EC50	EUbOPEN Chemogenomics Library - GPCR Dose-Respose
ChEMBL	Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay	F	7.37	pEC50	43	nM	EC50	J Med Chem (2021) 64: 5345-5364 [PMID:33524256]
ChEMBL	Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assay	F	7.4	pEC50	40	nM	EC50	J Med Chem (2021) 64: 5345-5364 [PMID:33524256]
ChEMBL	Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay	F	8.96	pEC50	1.1	nM	EC50	J Med Chem (2021) 64: 5345-5364 [PMID:33524256]
ChEMBL	Agonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilization	F	9.06	pEC50	0.87	nM	EC50	Bioorg Med Chem (2014) 22: 2992-2997 [PMID:24755525]
ChEMBL	Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis	F	10.3	pEC50	0.05	nM	EC50	J Med Chem (2021) 64: 18102-18113 [PMID:34855405]

ChEMBL data shown on this page come from version 35:

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]