laropiprant [Ligand Id: 3356] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL426559 (Cordaptive, Laropiprant, MK-0524) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| DP2 receptor/G protein-coupled receptor 44 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5071] [GtoPdb: 339] [UniProtKB: Q9Y5Y4] | ||||||||
| ChEMBL | Activity at CRTH2 receptor | B | 6.13 | pKi | 745 | nM | Ki | J Med Chem (2007) 50: 794-806 [PMID:17300164] |
| DP1 receptor/Prostanoid DP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258] | ||||||||
| ChEMBL | Binding affinity to human DP receptor expressed in HEK293 cells | B | 10.52 | pKd | 0.03 | nM | Kd | J Med Chem (2007) 50: 794-806 [PMID:17300164] |
| ChEMBL | Binding affinity to human DP receptor expressed in HEK293 cells | B | 9.24 | pKi | 0.57 | nM | Ki | J Med Chem (2007) 50: 794-806 [PMID:17300164] |
| ChEMBL | Activity at human DP receptor in platelet rich plasma assessed as inhibition of PGD2-induced cAMP accumulation | F | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2007) 50: 794-806 [PMID:17300164] |
| ChEMBL | Activity at sheep DP receptor by PRP assay | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2007) 50: 794-806 [PMID:17300164] |
| ChEMBL | Activity at human DP receptor in washed platelets assessed as inhibition of PGD2-induced cAMP accumulation | F | 10.05 | pIC50 | 0.09 | nM | IC50 | J Med Chem (2007) 50: 794-806 [PMID:17300164] |
| EP1 receptor/Prostanoid EP1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995] | ||||||||
| ChEMBL | Binding affinity to human EP1 receptor expressed in HEK293 cells | B | 5.94 | pKi | 1160 | nM | Ki | J Med Chem (2007) 50: 794-806 [PMID:17300164] |
| EP2 receptor/Prostanoid EP2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116] | ||||||||
| ChEMBL | Binding affinity to human EP2 receptor expressed in HEK293 cells | B | 6.87 | pKi | 136 | nM | Ki | J Med Chem (2007) 50: 794-806 [PMID:17300164] |
| EP3 receptor/Prostanoid EP3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115] | ||||||||
| ChEMBL | Binding affinity to human EP3 receptor expressed in HEK293 cells | B | 6.05 | pKi | 892 | nM | Ki | J Med Chem (2007) 50: 794-806 [PMID:17300164] |
| EP4 receptor/Prostanoid EP4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408] | ||||||||
| ChEMBL | Binding affinity to human EP4 receptor expressed in HEK293 cells | B | 4.82 | pKi | >15200 | nM | Ki | J Med Chem (2007) 50: 794-806 [PMID:17300164] |
| FP receptor/Prostanoid FP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1987] [GtoPdb: 344] [UniProtKB: P43088] | ||||||||
| ChEMBL | Binding affinity to human FP receptor expressed in HEK293 cells | B | 5 | pKi | 9991 | nM | Ki | J Med Chem (2007) 50: 794-806 [PMID:17300164] |
| IP receptor/Prostanoid IP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119] | ||||||||
| ChEMBL | Binding affinity to human IP receptor expressed in HEK293 cells | B | 5.18 | pKi | 6628 | nM | Ki | J Med Chem (2007) 50: 794-806 [PMID:17300164] |
| TP receptor/Thromboxane A2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069] [GtoPdb: 346] [UniProtKB: P21731] | ||||||||
| ChEMBL | Binding affinity to human TP receptor expressed in HEK293 cells | B | 7.96 | pKd | 10.9 | nM | Kd | J Med Chem (2007) 50: 794-806 [PMID:17300164] |
| GtoPdb | - | - | 6.1 | pKi | - | - | - | Clin Pharmacol Ther (2008) 83: 840-7 [PMID:17882161] |
| ChEMBL | Binding affinity to human TP receptor expressed in HEK293 cells | B | 8.53 | pKi | 2.95 | nM | Ki | J Med Chem (2007) 50: 794-806 [PMID:17300164] |
| ChEMBL | Activity at human TP receptor in platelet rich plasma assessed as inhibition U44619-induced platelet aggregation | F | 6.11 | pIC50 | 770 | nM | IC50 | J Med Chem (2007) 50: 794-806 [PMID:17300164] |
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]
