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Assay Detail

CHEMBL4773483

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

ADMET
Inhibition of human FKBP12 assessed as reduction in PPIase activity using succinyl-Ala-Leu-Pro-Phe-4-nitroanilide as substrate incubated for 4 mins by absorbance method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Targeting Protein Folding: A Novel Approach for the Treatment of Pathogenic Bacteria.
Scheuplein NJ,Bzdyl NM,Kibble EA,Lohr T,Holzgrabe U,Sarkar-Tyson M
J Med Chem (2020) 63 : 13355 -13388
PubMed 32786507 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.10 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4790993 1 6.75
CHEMBL4788177 1 6.72
CHEMBL4794577 1 6.66
CHEMBL4798300 1 5.92
CHEMBL4779246 1 4.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4790993 IC50 = 180.0 nM 6.75
CHEMBL4788177 IC50 = 190.0 nM 6.72
CHEMBL4794577 IC50 = 220.0 nM 6.66
CHEMBL4798300 IC50 = 1200.0 nM 5.92
CHEMBL4779246 IC50 = 36100.0 nM 4.44