apelin-13 [Ligand Id: 605] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL414173
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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 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 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]