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Assay Detail

CHEMBL678154

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity for FK506 binding protein 12 using [3H]-dihydro FK-506 radioligand was determined
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Peptidyl-prolyl cis-trans isomerase FKBP1A (CHEMBL1902)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

C32-O-imidazol-2-yl-methyl ether derivatives of the immunosuppressant ascomycin with improved therapeutic potential.
Goulet MT, McAlpine SR, Staruch MJ, Koprak S, Dumont FJ, Cryan JG, Wiederrecht GJ, Rosa R, Wilusz MB, Peterson LB, Wyvratt MJ, Parsons WH.
Bioorg Med Chem Lett (1998) 8 : 2253 -2258
PubMed 9873523 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 8.01 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8597 ASCOMYCIN 1 8.80
CHEMBL386482 1 8.13
CHEMBL385568 1 7.92
CHEMBL428499 1 7.66
CHEMBL262667 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8597 ASCOMYCIN EC50 = 1.6 nM 8.80
CHEMBL386482 EC50 = 7.4 nM 8.13
CHEMBL385568 EC50 = 12.0 nM 7.92
CHEMBL428499 EC50 = 22.0 nM 7.66
CHEMBL262667 EC50 = 30.0 nM 7.52