cligosiban [Ligand Id: 13229] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL594828 (PF-3274167) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ghrelin receptor/Ghrelin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4616] [GtoPdb: 246] [UniProtKB: Q92847] | ||||||||
| ChEMBL | Binding affinity to ghrelin receptor | B | 5.36 | pKi | 4400 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 516-520 [PMID:19963374] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Binding affinity to kappa opioid receptor | B | 5.52 | pKi | 3000 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 516-520 [PMID:19963374] |
| NK1 receptor/Neurokinin 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103] | ||||||||
| ChEMBL | Binding affinity to NK1 receptor | B | 5.19 | pKi | 6500 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 516-520 [PMID:19963374] |
| OT receptor/Oxytocin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2049] [GtoPdb: 369] [UniProtKB: P30559] | ||||||||
| ChEMBL | Antagonist activity at human cloned oxytocin receptor by cell based beta lactamase assay | F | 8.02 | pKi | 9.5 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 516-520 [PMID:19963374] |
| ChEMBL | Displacement of [3H]-oxytocin from oxytocin receptor in human uterus tissue | B | 8.02 | pKi | 9.5 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| ChEMBL | Displacement of [3H]-oxytocin from human oxytocin receptor expressed in HEK293-EBNA cells | B | 8.02 | pKi | 9.5 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| ChEMBL | Antagonist activity at human OTR receptor expressed in HEK293FT cells assessed as inhibition of LIT-001-induced calcium release by Aequorin based assay | F | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| ChEMBL | Antagonist activity at human OTR receptor expressed in HEK293FT cells assessed as inhibition of LIT-001-induced response incubated for 30 mins by beta-arrestin recruitment assay | F | 7.2 | pIC50 | 63 | nM | IC50 | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| ChEMBL | Antagonist activity at human OTR expressed in HEK293 cells assessed as decrease in calcium flux measured after 10 mins in presence of vasopressin by Fluo-4 dye based microplate reader based assay | F | 7.63 | pIC50 | 23.2 | nM | IC50 | ACS Med Chem Lett (2019) 10: 996-1001 [PMID:31223461] |
| V1A receptor/Vasopressin V1a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288] | ||||||||
| ChEMBL | Antagonist activity at human cloned vasopressin V1a receptor by cell based beta lactamase assay | F | 5.95 | pKi | 1120 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 516-520 [PMID:19963374] |
| ChEMBL | Displacement of [3H]vasopressin from human vasopressin V1a receptor expressed in CHO cells at 10 uM | B | 5.95 | pKi | 1120 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| V1B receptor/Vasopressin V1b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1921] [GtoPdb: 367] [UniProtKB: P47901] | ||||||||
| ChEMBL | Displacement of [3H]vasopressin from human vasopressin V1b receptor expressed in CHO cells | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| V2 receptor/Vasopressin V2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1790] [GtoPdb: 368] [UniProtKB: P30518] | ||||||||
| ChEMBL | Antagonist activity at human cloned vasopressin V2 receptor by cell based beta lactamase assay | F | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 516-520 [PMID:19963374] |
| ChEMBL | Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| ChEMBL | Antagonist activity at human V2 receptor expressed in HEK293FT cells assessed as inhibition of LIT-001-induced response incubated for 30 mins by beta-arrestin recruitment assay | F | 5.58 | pIC50 | 2620 | nM | IC50 | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| ChEMBL | Antagonist activity at human V2 receptor expressed in HEK293FT cells assessed as inhibition of AVP-induced calcium release by Aequorin based assay | F | 5.82 | pIC50 | 1530 | nM | IC50 | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
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]
