AC264613 [Ligand Id: 9460] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL494502 (AC-264613) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| ChEMBL | PDSP Secondary Binding target: HRH1 - 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 | 5.7 | pKi | 1979.7 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | PDSP Secondary Binding target: OPRM1 - 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 | pKi | >10000 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| PAR2/Proteinase-activated receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5963] [GtoPdb: 348] [UniProtKB: P55085] | ||||||||
| ChEMBL | Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2008) 51: 5490-5493 [PMID:18720984] |
| GtoPdb | - | - | 7.5 | pEC50 | 31.6 | nM | EC50 | J Med Chem (2008) 51: 5490-3 [PMID:18720984] |
| ChEMBL | Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay | F | 7.5 | pEC50 | 31.62 | nM | EC50 | J Med Chem (2008) 51: 5490-5493 [PMID:18720984] |
| ChEMBL | Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay | F | 7.5 | pEC50 | 31.62 | nM | EC50 | J Med Chem (2008) 51: 5490-5493 [PMID:18720984] |
| ChEMBL | Agonist activity at human PAR2 expressed in HEK293T cells assessed as increase in intracellular calcium level by bioluminescence assay | F | 7.52 | pEC50 | 30 | nM | EC50 | J Med Chem (2013) 56: 7477-7497 [PMID:23895492] |
| ChEMBL | Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of phosphatidylinositol hydrolysis after 45 mins by scintillation counting analysis | F | 7.52 | pEC50 | 30 | nM | EC50 | J Med Chem (2013) 56: 7477-7497 [PMID:23895492] |
| ChEMBL | Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assay | B | 7.52 | pEC50 | 30 | nM | EC50 | J Med Chem (2013) 56: 7477-7497 [PMID:23895492] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | PDSP Secondary Binding target: HTR2A - 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 | 5.41 | pKi | 3878.82 | 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]
