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Assay Detail

CHEMBL5629798

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

Binding
Binding affinity to human FKBP51 FK1 domain expressed in Escherichia coli BL21 DE3 Gold assessed as dissociation constant incubated for 30 mins by competitive fluorescence polarization assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Peptidyl-prolyl cis-trans isomerase FKBP5 (CHEMBL2052031)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Antascomicin B stabilizes FKBP51-Akt1 complexes as a molecular glue.
Schäfer SC, Voll AM, Bracher A, Ley SV, Hausch F.
Bioorg Med Chem Lett (2024) 104 : 129728 -129728
PubMed 38582133 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 7.79 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5634031 1 8.17
CHEMBL413 SIROLIMUS 4.0 1 8.07
CHEMBL269732 TACROLIMUS ANHYDROUS 4.0 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5634031 Kd = 6.7 nM 8.17
CHEMBL413 SIROLIMUS Kd = 8.5 nM 8.07
CHEMBL269732 TACROLIMUS ANHYDROUS Kd = 75.93 nM 7.12