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ChEMBL ligand: CHEMBL6367 (GPI-1046) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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FKBP prolyl isomerase 1A/FK506-binding protein 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1902] [GtoPdb: 2609] [UniProtKB: P62942] | ||||||||
ChEMBL | Binding affinity to FKBP12 (unknown origin) | B | 6.51 | pKi | 306 | nM | Ki | J Med Chem (2016) 59: 9622-9644 [PMID:27409354] |
ChEMBL | Inhibitory activity against FK506 binding protein 12 | B | 8.12 | pKi | 7.5 | nM | Ki | J Med Chem (2002) 45: 3549-3557 [PMID:12139466] |
ChEMBL | The compound was tested for binding affinity against rotamase | B | 8.12 | pKi | 7.5 | nM | Ki | J Med Chem (1998) 41: 3928-3939 [PMID:9767630] |
ChEMBL | Binding affinity to FKBP12 (unknown origin) | B | 8.12 | pKi | 7.5 | nM | Ki | J Med Chem (2016) 59: 9622-9644 [PMID:27409354] |
ChEMBL | Ability to inhibit peptidyl-prolyl isomerase (PPIase, or rotamase) activity of FK506 binding protein 12 | B | 11 | pKi | 0.01 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1429-1433 [PMID:11992791] |
ChEMBL | Binding affinity to FKBP12 by fluorescence polarization assay | B | 5.91 | pIC50 | 1240 | nM | IC50 | J Med Chem (2012) 55: 4114-4122 [PMID:22455444] |
FKBP prolyl isomerase 1A/FK506-binding protein 1A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2095] [GtoPdb: 2609] [UniProtKB: Q62658] | ||||||||
ChEMBL | In vitro inhibition of rotamase activity of FK506 binding protein 12 | B | 8.12 | pKi | 7.5 | nM | Ki | J Med Chem (2002) 45: 3558-3568 [PMID:12139467] |
FKBP prolyl isomerase 4/FK506 binding protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4050] [GtoPdb: 3176] [UniProtKB: Q02790] | ||||||||
ChEMBL | Binding affinity to FKBP52 (unknown origin) | B | 6.03 | pKi | 936 | nM | Ki | J Med Chem (2016) 59: 9622-9644 [PMID:27409354] |
ChEMBL | Binding affinity to FKBP52 FK1 domain by fluorescence polarization assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 4114-4122 [PMID:22455444] |
FKBP prolyl isomerase 5/Peptidyl-prolyl cis-trans isomerase FKBP5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2052031] [GtoPdb: 3175] [UniProtKB: Q13451] | ||||||||
ChEMBL | Binding affinity to FKBP51 (unknown origin) | B | 6.35 | pKi | 447 | nM | Ki | J Med Chem (2016) 59: 9622-9644 [PMID:27409354] |
ChEMBL | Binding affinity to FKBP51 FK1 domain by fluorescence polarization assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 4114-4122 [PMID:22455444] |
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345] | ||||||||
ChEMBL | The inhibitory activity by using FK506 binding protein 12 SPA binding assay | B | 4.68 | pIC50 | 20892.96 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 1007-1010 [PMID:10843203] |
FKBP prolyl isomerase 8 in Human [GtoPdb: 3177] [UniProtKB: Q14318] | ||||||||
GtoPdb | - | - | 7.32 | pKi | 48 | nM | Ki | J Biol Chem (2006) 281: 14961-70 [PMID:16547004] |
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]