TRV023   Click here for help

GtoPdb Ligand ID: 11943

Synonyms: TRV 023 | TRV-023
Comment: TRV023 is an angiotensin II (AngII) analogue, in which the C-terminal Phe8 residue is replaced with Ala [2]. This modification attenuates Gq-mediated signalling, but has no effect of β-arrestin-dependent receptor endocytosis.
Click here for help
2D Structure
Click here for help
Click here for structure editor
Click here for help
Canonical SMILES NCCCCC(C(=O)NC(C(=O)N1CCCC1C(=O)NC(C(=O)O)C)Cc1[nH]cnc1)NC(=O)C(NC(=O)C(C(C)C)NC(=O)C(NC(=O)CNC)CCCN=C(N)N)Cc1ccc(cc1)O
Isomeric SMILES CC(C)C(C(=O)NC(Cc1ccc(cc1)O)C(=O)NC(CCCCN)C(=O)NC(Cc1cnc[nH]1)C(=O)N1CCCC1C(=O)NC(C)C(=O)O)NC(=O)C(CCCN=C(N)N)NC(=O)CNC
InChI InChI=1S/C43H68N14O10/c1-24(2)35(56-37(61)29(52-34(59)22-47-4)10-7-17-49-43(45)46)40(64)54-31(19-26-12-14-28(58)15-13-26)38(62)53-30(9-5-6-16-44)36(60)55-32(20-27-21-48-23-50-27)41(65)57-18-8-11-33(57)39(63)51-25(3)42(66)67/h12-15,21,23-25,29-33,35,47,58H,5-11,16-20,22,44H2,1-4H3,(H,48,50)(H,51,63)(H,52,59)(H,53,62)(H,54,64)(H,55,60)(H,56,61)(H,66,67)(H4,45,46,49)
Selectivity at GPCRs
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
AT1 receptor Hs Agonist Biased agonist 8.6 pKi - 1
pKi 8.6 [1]
Description: Receptor binding
AT1 receptor Hs Agonist Biased agonist 5.7 pEC50 - 3
pEC50 5.7 (EC50 2.1x10-6 M) [3]
Description: β-arrestin recruitment assay