SAFit2 [Ligand Id: 11482] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3623630 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | GPCRScan assay: inhibition of D2 | B | 5 | pKi | >10000 | nM | Ki | Data for DCP probe SAFit2 |
| FKBP prolyl isomerase 1A/FK506-binding protein 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1902] [GtoPdb: 2609] [UniProtKB: P62942] | ||||||||
| ChEMBL | Competitive fluorescence polarization binding assay (FKBP1A) | B | 6.93 | pKd | 116.4 | nM | Kd | Data for DCP probe SAFit2 |
| ChEMBL | NanoBRET assay (FKBP51-NLuc) (FKBP1A) | B | 5.96 | pIC50 | 1103 | nM | IC50 | Data for DCP probe SAFit2 |
| ChEMBL | NanoBRET assay (FKBP12-NLuc) (FKBP1A) | B | 6.11 | pIC50 | 771 | nM | IC50 | Data for DCP probe SAFit2 |
| FK506-binding protein 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2430] [UniProtKB: P68106] | ||||||||
| ChEMBL | Competitive fluorescence polarization binding assay (FKBP1B) | B | 7.41 | pKd | 38.9 | nM | Kd | Data for DCP probe SAFit2 |
| ChEMBL | NanoBRET assay (FKBP12-NLuc) (FKBP1B) | B | 7.1 | pIC50 | 80 | nM | IC50 | Data for DCP probe SAFit2 |
| FKBP prolyl isomerase 4/FK506 binding protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4050] [GtoPdb: 3176] [UniProtKB: Q02790] | ||||||||
| ChEMBL | NanoBRET assay (FKBP12-NLuc) (FKBP4) | B | 5.85 | pIC50 | 1409 | nM | IC50 | Data for DCP probe SAFit2 |
| H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8] | ||||||||
| ChEMBL | GPCRScan assay: inhibition of H4 | B | 5.47 | pKi | 3382 | nM | Ki | Data for DCP probe SAFit2 |
| Peptidyl-prolyl cis-trans isomerase FKBP2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105949] [UniProtKB: P26885] | ||||||||
| ChEMBL | Competitive fluorescence polarization binding assay (FKBP2) | B | 5.98 | pKd | 1053 | nM | Kd | Data for DCP probe SAFit2 |
| FKBP prolyl isomerase 5/Peptidyl-prolyl cis-trans isomerase FKBP5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2052031] [GtoPdb: 3175] [UniProtKB: Q13451] | ||||||||
| ChEMBL | Competitive fluorescence polarization binding assay (FKBP5) | B | 8.22 | pKd | 6 | nM | Kd | Data for DCP probe SAFit2 |
| GtoPdb | - | - | 8.22 | pKi | 6 | nM | Ki | Nat Chem Biol (2015) 11: 33-7 [PMID:25436518] |
| ChEMBL | Displacement of iFit-FL from FKBP51 (unknown origin) by fluorescence polarization assay | B | 8.22 | pKi | 6 | nM | Ki | J Med Chem (2015) 58: 7796-7806 [PMID:26419422] |
| ChEMBL | Binding affinity to FKBP51 (unknown origin) by competitive fluorescence polarization assay | B | 8.22 | pKi | 6 | nM | Ki | J Med Chem (2016) 59: 2410-2422 [PMID:26954324] |
| ChEMBL | NanoBRET assay (FKBP51-NLuc) (FKBP5) | B | 6.31 | pIC50 | 493 | nM | IC50 | Data for DCP probe SAFit2 |
| ChEMBL | NanoBRET assay (FKBP12-NLuc) | B | 6.71 | pIC50 | 195.5 | nM | IC50 | Data for DCP probe SAFit2 |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | GPCRScan assay: inhibition of 5-HT2C | B | 5 | pKi | >10000 | nM | Ki | Data for DCP probe SAFit2 |
| σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2] | ||||||||
| ChEMBL | GPCRScan assay: inhibition of Sigma 2 | B | 6.65 | pKi | 226 | nM | Ki | Data for DCP probe SAFit2 |
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]
