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 |
|---|---|---|---|---|---|---|---|---|
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | PDSP Secondary Binding target: DRD3 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.95 | pKi | 1122.15 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| 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] |
| Translocator protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5742] [GtoPdb: 2879] [UniProtKB: P30536] | ||||||||
| ChEMBL | PDSP Secondary Binding target: TSPO - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.54 | pKi | 286.42 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
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]
