palupiprant [Ligand Id: 14139] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3670685 (E 7046, Er-886046, ER 886046, Palupiprant) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| EP1 receptor/Prostanoid EP1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995] | ||||||||
| ChEMBL | Antagonist activity at human EP1 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2020) 63: 569-590 [PMID:31855426] |
| ChEMBL | Antagonist activity at human EP1 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7896-7917 [PMID:35640059] |
| ChEMBL | Antagonist activity at EP1 receptor (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | ACS Med Chem Lett (2023) 14: 727-736 [PMID:37312837] |
| EP2 receptor/Prostanoid EP2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116] | ||||||||
| ChEMBL | Antagonist activity at human EP2 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2020) 63: 569-590 [PMID:31855426] |
| ChEMBL | Antagonist activity at human EP2 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7896-7917 [PMID:35640059] |
| ChEMBL | Antagonist activity at EP2 receptor (unknown origin) | B | 6.03 | pIC50 | 928.2 | nM | IC50 | ACS Med Chem Lett (2023) 14: 727-736 [PMID:37312837] |
| EP3 receptor/Prostanoid EP3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115] | ||||||||
| ChEMBL | Antagonist activity at human EP3 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2020) 63: 569-590 [PMID:31855426] |
| ChEMBL | Antagonist activity at human EP3 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7896-7917 [PMID:35640059] |
| ChEMBL | Antagonist activity at EP3 receptor (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | ACS Med Chem Lett (2023) 14: 727-736 [PMID:37312837] |
| EP4 receptor/Prostanoid EP4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408] | ||||||||
| ChEMBL | Radioligand Binding Assay:: The radioligand EP4 binding assay was performed using ChemiScreen recombinant human EP4 receptor membrane preparations from Millipore, according to manufacturer's instructions. Briefly, membranes prepared from Chem-1 cells overexpressing human EP4 cDNA (Millipore) were mixed with 1.8 nmol.L−1 [3H]-PGE2 and 5 μmol.L−1 unlabelled PGE2 in the presence or absence of various concentrations of testing compounds in binding buffer (50 mmol.L−1 HEPES, pH 7.4, 5 mmol.L−1 MgCl2, 1 mmol.L−1 CaCl2, 0.2% BSA) in a nonbinding 96-well plate, and incubated for 1-2 h at room temperature. Prior to filtration, a GF/C 96-well filter plate was coated with 0.33% polyethyleneimine for 30 min, then washed with 50 mmol.L−1 HEPES, pH 7.4, 0.5% BSA. Binding reactions were transferred to the filter plate, and washed 3 times with Wash Buffer (1 mL per well per wash). | B | 8.1 | pKi | 8 | nM | Ki | US-8686018-B2. Pharmaceutical composition (2014) |
| GtoPdb | - | - | 8.2 | pKi | - | - | - |
Oncoimmunology (2017) 6: e1338239 [PMID:28920002]; J Immunother Cancer (2020) 8: [PMID:32554609] |
| ChEMBL | Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced cAMP production measured for 30 mins by Glosensor cAMP assay | F | 7.6 | pIC50 | 25.3 | nM | IC50 | J Med Chem (2023) 66: 6218-6238 [PMID:36880691] |
| ChEMBL | Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as reduction in PGE2-mediated cAMP accumulation preincubated for 30 mins followed by PEG2 addition by GloSensor cAMP assay | F | 7.73 | pIC50 | 18.5 | nM | IC50 | J Med Chem (2022) 65: 7896-7917 [PMID:35640059] |
| ChEMBL | Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced CRE-mediated gene transcription preincubated with compound followed by PGE2 stimulation and measured after 12 hrs by firefly luciferase assay | F | 7.8 | pIC50 | 15.7 | nM | IC50 | J Med Chem (2023) 66: 6218-6238 [PMID:36880691] |
| ChEMBL | Antagonist activity at EP4 receptor (unknown origin) | B | 7.87 | pIC50 | 13.5 | nM | IC50 | ACS Med Chem Lett (2023) 14: 727-736 [PMID:37312837] |
| ChEMBL | Antagonist activity at human EP4 receptor overexpressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP formation preincubated for 15 mins followed by PGE addition and measured after 30 mins by Eu-cAMP tracer based assay | F | 8 | pIC50 | 10.1 | nM | IC50 | ACS Med Chem Lett (2023) 14: 727-736 [PMID:37312837] |
| ChEMBL | Antagonist activity at human EP4 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay | F | 8.12 | pIC50 | 7.5 | nM | IC50 | J Med Chem (2020) 63: 569-590 [PMID:31855426] |
| ChEMBL | Antagonist activity at human EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay | F | 8.12 | pIC50 | 7.5 | nM | IC50 | J Med Chem (2022) 65: 7896-7917 [PMID:35640059] |
| ChEMBL | Antagonist activity at human EP4 receptor transfected in HEK293 cells assessed as inhibition of PGE2-induced beta-arrestin recruitment preincubated with compound for 20 mins followed by PGE2 stimulation and measured after 12 hrs by Tango assay | F | 8.35 | pIC50 | 4.5 | nM | IC50 | J Med Chem (2023) 66: 6218-6238 [PMID:36880691] |
| EP4 receptor/Prostanoid EP4 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2489] [GtoPdb: 343] [UniProtKB: P32240] | ||||||||
| ChEMBL | Antagonist activity at mouse EP4 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay | F | 6.74 | pIC50 | 181.1 | nM | IC50 | J Med Chem (2020) 63: 569-590 [PMID:31855426] |
| ChEMBL | Antagonist activity at mouse EP4 receptor transfected in CHO/Galpha16 cells preincubated for 15 mins followed by PGE2 addition by calcium flux assay | F | 6.99 | pIC50 | 101.2 | nM | IC50 | J Med Chem (2022) 65: 7896-7917 [PMID:35640059] |
ChEMBL data shown on this page come from version 35:
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]
