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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 |
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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 | 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 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]