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Assay Detail

CHEMBL678142

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

Binding
The compound was tested for binding affinity against human FK506 binding protein 12
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

Retention of immunosuppressant activity in an ascomycin analogue lacking a hydrogen-bonding interaction with FKBP12.
Wiedeman PE, Fesik SW, Petros AM, Nettesheim DG, Mollison KW, Lane BC, Or YS, Luly JR.
J Med Chem (1999) 42 : 4456 -4461
PubMed 10543889 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.18 9.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL71458 1 9.11
CHEMBL8597 ASCOMYCIN 1 8.68
CHEMBL269732 TACROLIMUS ANHYDROUS 4.0 1 8.64
CHEMBL139966 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL71458 IC50 = 0.77 nM 9.11
CHEMBL8597 ASCOMYCIN IC50 = 2.1 nM 8.68
CHEMBL269732 TACROLIMUS ANHYDROUS IC50 = 2.3 nM 8.64
CHEMBL139966 IC50 = 529.0 nM 6.28