L-368,899 [Ligand Id: 2249] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL1253853
There should be some charts here, you may need to enable JavaScript!
  • V1A receptor/Vasopressin V1a receptor in Human [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288]
  • V1A receptor/Vasopressin V1a receptor in Rat [ChEMBL: CHEMBL2868] [GtoPdb: 366] [UniProtKB: P30560]
There should be some charts here, you may need to enable JavaScript!
  • V2 receptor/Vasopressin V2 receptor in Human [ChEMBL: CHEMBL1790] [GtoPdb: 368] [UniProtKB: P30518]
  • V2 receptor/Vasopressin V2 receptor in Rat [ChEMBL: CHEMBL3766] [GtoPdb: 368] [UniProtKB: Q00788]
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
OT receptor/Oxytocin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2049] [GtoPdb: 369] [UniProtKB: P30559]
ChEMBL Displacement of [3H]-oxytocin from oxytocin receptor in human uterus tissue B 7.89 pKi 13 nM Ki J Med Chem (2010) 53: 6525-6538 [PMID:20550119]
ChEMBL Binding affinity to human OT receptor B 7.89 pKi 13 nM Ki Bioorg Med Chem Lett (2013) 23: 902-906 [PMID:23270988]
GtoPdb - - 8.1 pKi - - - Life Sci (1995) 57: 2253-61 [PMID:7475979]
OT receptor/Oxytocin receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3996] [GtoPdb: 369] [UniProtKB: P70536]
ChEMBL Displacement of [3H]-oxytocin from oxytocin receptor in rat uterus tissue B 8.44 pKi 3.6 nM Ki J Med Chem (2010) 53: 6525-6538 [PMID:20550119]
ChEMBL Inhibition of rat uterus OT receptor B 8.05 pIC50 8.9 nM IC50 Bioorg Med Chem Lett (2013) 23: 902-906 [PMID:23270988]
V1A receptor/Vasopressin V1a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288]
ChEMBL Displacement of [3H]vasopressin from vasopressin V1a receptor in human liver tissue B 6.74 pKi 180 nM Ki J Med Chem (2010) 53: 6525-6538 [PMID:20550119]
ChEMBL Binding affinity to human liver V1A receptor B 6.74 pKi 180 nM Ki Bioorg Med Chem Lett (2013) 23: 902-906 [PMID:23270988]
V1A receptor/Vasopressin V1a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2868] [GtoPdb: 366] [UniProtKB: P30560]
ChEMBL Displacement of [3H]vasopressin from vasopressin V1a receptor in rat liver tissue B 6.96 pKi 110 nM Ki J Med Chem (2010) 53: 6525-6538 [PMID:20550119]
ChEMBL Inhibition of rat liver V1a receptor B 6.43 pIC50 370 nM IC50 Bioorg Med Chem Lett (2013) 23: 902-906 [PMID:23270988]
V2 receptor/Vasopressin V2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1790] [GtoPdb: 368] [UniProtKB: P30518]
ChEMBL Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue B 6.23 pKi 590 nM Ki J Med Chem (2010) 53: 6525-6538 [PMID:20550119]
ChEMBL Binding affinity to human V2 receptor B 6.23 pKi 590 nM Ki Bioorg Med Chem Lett (2013) 23: 902-906 [PMID:23270988]
V2 receptor/Vasopressin V2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3766] [GtoPdb: 368] [UniProtKB: Q00788]
ChEMBL Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue B 6.7 pKi 200 nM Ki J Med Chem (2010) 53: 6525-6538 [PMID:20550119]
ChEMBL Inhibition of rat kidney V2 receptor B 6.24 pIC50 570 nM IC50 Bioorg Med Chem Lett (2013) 23: 902-906 [PMID:23270988]

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]