GAT100 [Ligand Id: 9237] activity data from GtoPdb
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CB1 receptor in Human [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
| GtoPdb | Measuring GAT100's inhibition of [3H]SR141716A binding, in radioligand binding assays | - | 6.39 | pEC50 | 409.8 | nM | EC50 | ACS Chem Neurosci (2016) 7: 776-98 [PMID:27046127] |
| GtoPdb | Although GAT100 antagonized CP55940-induced stimulation of [35S]GTPγS binding to human CB1 CHO cell membranes, it enhanced the binding of [3H]CP55940 to these membranes. The EC50 and Emax values of GAT100 for this enhancement, with the 95% confidence limits shown in brackets, were 19.6 nM (10.4 & 36.9 nM) and 116.5% (108.3 & 124.6%), respectively. GAT100 (500 nM) was also found to enhance saturation binding of [3H]CP55940 to human CB1 HEK293 cell membranes. | - | 7.72 | pEC50 | 19.2 | nM | EC50 | J Med Chem (2016) 59: 44-60 [PMID:26529344] |
Our curators have not yet identified this ligand in ChEMBL, but you may find additional data by searching on the ChEMBL site using the ligand's name or structure.
