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Assay Detail

CHEMBL678150

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

Binding
Ability to bind the major cystolic receptor FK506 binding protein 12 by using competitive binding assay
4
Total Activities
4
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

Alkyl ether analogs of the FK-506 related, immunosuppressive macrolide L-683,590 (ascomycin)
Goulet MT, Hodkey DW, Staruch MJ, Dumont FJ, Cryan JG, Parsons WH, Wyvratt MJ
Bioorg Med Chem Lett (1994) 4 : 921 -926
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.90 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8597 ASCOMYCIN 1 8.80
CHEMBL384325 1 7.69
CHEMBL262492 1 7.64
CHEMBL406510 1 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8597 ASCOMYCIN EC50 = 1.6 nM 8.80
CHEMBL384325 EC50 = 20.5 nM 7.69
CHEMBL262492 EC50 = 23.0 nM 7.64
CHEMBL406510 EC50 = 34.3 nM 7.46