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Assay Detail

CHEMBL4835130

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Binding
Binding affinity to FKBP51 FK1 domain (unknown origin) assessed as dissociation constant at 25 degreeC by isothermal titration calorimetric analysis
2
Total Activities
2
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

Structure-Based Design of High-Affinity Macrocyclic FKBP51 Inhibitors.
Bauder M, Meyners C, Purder PL, Merz S, Sugiarto WO, Voll AM, Heymann T, Hausch F.
J Med Chem (2021) 64 : 3320 -3349
PubMed 33666419 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 8.09 8.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4871144 1 8.16
CHEMBL3623612 1 8.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4871144 Kd = 6.9 nM 8.16
CHEMBL3623612 Kd = 9.8 nM 8.01