ChEMBL ligand: CHEMBL269732 (FK-506, FK506, FR-900506, NSC-758659, Prograf, Protopic, Tacrolimus, Tacrolimus monohydrate)
CYP3A4/Cytochrome P450 3A4 in Human [ChEMBL: CHEMBL340] [GtoPdb: 1337] [UniProtKB: P08684] There should be some charts here, you may need to enable JavaScript!
FKBP prolyl isomerase 1A/FK506-binding protein 1A in Human [ChEMBL: CHEMBL1902] [GtoPdb: 2609] [UniProtKB: P62942] There should be some charts here, you may need to enable JavaScript!
FK506-binding protein 1B in Human [ChEMBL: CHEMBL2430] [UniProtKB: P68106] There should be some charts here, you may need to enable JavaScript!
FKBP prolyl isomerase 5/Peptidyl-prolyl cis-trans isomerase FKBP5 in Human [ChEMBL: CHEMBL2052031] [GtoPdb: 3175] [UniProtKB: Q13451] There should be some charts here, you may need to enable JavaScript!
Plasmodium falciparum [ChEMBL: CHEMBL364] There should be some charts here, you may need to enable JavaScript!
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345] There should be some charts here, you may need to enable JavaScript!
Serine/threonine protein phosphatase 2B catalytic subunit, alpha isoform in Human [ChEMBL: CHEMBL4445] [UniProtKB: Q08209] There should be some charts here, you may need to enable JavaScript!
OATP1B1/Solute carrier organic anion transporter family member 1B1 in Human [ChEMBL: CHEMBL1697668] [GtoPdb: 1220] [UniProtKB: Q9Y6L6] There should be some charts here, you may need to enable JavaScript!
Splicing factor 3B subunit 3 in Human [ChEMBL: CHEMBL1250378] [UniProtKB: Q15393] There should be some charts here, you may need to enable JavaScript!
TRPM8 in Human [GtoPdb: 500] [UniProtKB: Q7Z2W7] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
CYP3A4/Cytochrome P450 3A4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL340] [GtoPdb: 1337] [UniProtKB: P08684]
ChEMBL	DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin)	B	6	pIC50	1000	nM	IC50	DrugMatrix in vitro pharmacology data
FKBP prolyl isomerase 1A/FK506-binding protein 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1902] [GtoPdb: 2609] [UniProtKB: P62942]
ChEMBL	Binding affinity to FK506 binding protein 12 was determined	B	9.7	pKd	0.2	nM	Kd	Bioorg Med Chem Lett (1995) 5: 2341-2346
ChEMBL	The compound was evaluated for its affinity to the binding domain of immunophilin FK506 binding protein 12	B	9.7	pKd	0.2	nM	Kd	Bioorg Med Chem Lett (1993) 3: 1947-1950
ChEMBL	Compound was tested for its ability to inhibit FK506 binding protein 12 rotamase activity	B	9.4	pKi	0.4	nM	Ki	J Med Chem (1998) 41: 5119-5143 [PMID:9857082]
GtoPdb	-	-	9.4	pKi	0.4	nM	Ki	J Med Chem (1998) 41: 5119-43 [PMID:9857082]
ChEMBL	Binding affinity to FKBP12 (unknown origin) expressed in HEK293 cells co-expressing FRB assessed as inhibition of rapamycin-induced FKBP12-FRB dimerization measured after 25 mins by nano-glo live cell reagent based luminescence assay	B	4.42	pIC50	38290	nM	IC50	Eur J Med Chem (2021) 213: 113160-113160 [PMID:33493827]
ChEMBL	Binding affinity towards recombinant FK506 binding protein 12 to determine the FKBP binding property of the compound	B	6	pIC50	1000	nM	IC50	J Med Chem (1981) 24: 496-499 [PMID:7241506]
ChEMBL	Antagonist activity at human FKBP12 measured after 30 mins by fluorescein labelled SLF tracer based fluorescence polarization assay	B	7.85	pIC50	14.05	nM	IC50	Bioorg Med Chem Lett (2017) 27: 2465-2471 [PMID:28412204]
ChEMBL	Inhibitory binding activity against human Immunophilin-FK-506 binding protein 12	B	8.6	pIC50	2.5	nM	IC50	J Med Chem (1998) 41: 1764-1776 [PMID:9599228]
ChEMBL	The compound was tested for binding affinity against human FK506 binding protein 12	B	8.64	pIC50	2.3	nM	IC50	J Med Chem (1999) 42: 4456-4461 [PMID:10543889]
ChEMBL	Effective concentration against FK506 binding protein 12 using [3H]-dihydro FK-506	B	9.05	pEC50	0.9	nM	EC50	Bioorg Med Chem Lett (1999) 9: 2089-2094 [PMID:10450987]
FK506-binding protein 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2430] [UniProtKB: P68106]
ChEMBL	Binding affinity to FKBP12 (unknown origin) by NMR analysis	B	9.4	pKd	0.4	nM	Kd	J Med Chem (2014) 57: 7819-7837 [PMID:24913411]
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 human FKBP51 by competitive fluorescence polarization assay	B	7.1	pKi	80	nM	Ki	J Med Chem (2013) 56: 3922-3935 [PMID:23647266]
ChEMBL	Binding affinity to FKBP51 (unknown origin) by competitive fluorescence polarization assay	B	7.1	pKi	79	nM	Ki	J Med Chem (2016) 59: 2410-2422 [PMID:26954324]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL	Antiplasmodial activity against blood stage of Plasmodium falciparum 3D7 assessed as parasite growth inhibition	F	5.72	pIC50	1900	nM	IC50	ACS Med Chem Lett (2020) 11: 2131-2138 [PMID:33209191]
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	8.5	pIC50	3.16	nM	IC50	Bioorg Med Chem Lett (2000) 10: 1007-1010 [PMID:10843203]
ChEMBL	Inhibitory activity against macrophilin (FKBP-12)	B	9.02	pIC50	0.95	nM	IC50	J Med Chem (2004) 47: 4950-4957 [PMID:15369399]
Serine/threonine protein phosphatase 2B catalytic subunit, alpha isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4445] [UniProtKB: Q08209]
ChEMBL	Binding affinity to protein phosphatase, calcineurin (CN) was determined	B	7.7	pKd	20	nM	Kd	Bioorg Med Chem Lett (1995) 5: 2341-2346
ChEMBL	Inhibitory activity against Calcineurin (CaN phosphatase)	B	7.83	pIC50	14.8	nM	IC50	Bioorg Med Chem Lett (1999) 9: 2089-2094 [PMID:10450987]
OATP1B1/Solute carrier organic anion transporter family member 1B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697668] [GtoPdb: 1220] [UniProtKB: Q9Y6L6]
ChEMBL	TP_TRANSPORTER: inhibition of Phalloidin uptake (Phalloidin: 1 uM) in OATP-C-expressing HEK293 cells	F	5.43	pIC50	3700	nM	IC50	Naunyn Schmiedebergs Arch Pharmacol (2003) 368: 415-420 [PMID:14530907]
Splicing factor 3B subunit 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1250378] [UniProtKB: Q15393]
ChEMBL	Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay	B	7.86	pIC50	13.8	nM	IC50	Nat Chem Biol (2007) 3: 570-575 [PMID:17643112]
ChEMBL	Inhibition of SAP130 mediated cell growth in human WiDr cells	B	7.96	pIC50	10.9	nM	IC50	Nat Chem Biol (2007) 3: 570-575 [PMID:17643112]
TRPM8 in Human [GtoPdb: 500] [UniProtKB: Q7Z2W7]
GtoPdb	FURA2AM experiments, human TRPM8	-	4.85	pEC50	14100	nM	EC50	J Neurosci (2019) 39: 949-969 [PMID:30545944]

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]