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Assay Detail

CHEMBL1657166

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

Binding
Inhibition of PPIase activity of human FKBP12 expressed in Escherichia coli by spectrophotometry
13
Total Activities
13
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 FKBP1A (CHEMBL1902)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein.
Juli C, Sippel M, Jäger J, Thiele A, Weiwad M, Schweimer K, Rösch P, Steinert M, Sotriffer CA, Holzgrabe U.
J Med Chem (2011) 54 : 277 -283
PubMed 21142106 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.31 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1650949 1 7.16
CHEMBL1650947 1 6.92
CHEMBL1650948 1 6.82
CHEMBL1650946 1 6.70
CHEMBL109278 1 6.70
CHEMBL1650943 1 6.58
CHEMBL1650950 1 6.50
CHEMBL1650803 1 5.58
CHEMBL1650805 1 5.55
CHEMBL1650804 1 5.51
CHEMBL1650945 1 5.38
CHEMBL1650802 1 -
CHEMBL1650944 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1650949 IC50 = 70.0 nM 7.16
CHEMBL1650947 IC50 = 120.0 nM 6.92
CHEMBL1650948 IC50 = 150.0 nM 6.82
CHEMBL1650946 IC50 = 200.0 nM 6.70
CHEMBL109278 IC50 = 200.0 nM 6.70
CHEMBL1650943 IC50 = 260.0 nM 6.58
CHEMBL1650950 IC50 = 320.0 nM 6.50
CHEMBL1650803 IC50 = 2600.0 nM 5.58
CHEMBL1650805 IC50 = 2800.0 nM 5.55
CHEMBL1650804 IC50 = 3100.0 nM 5.51
CHEMBL1650945 IC50 = 4200.0 nM 5.38
CHEMBL1650802 IC50 > 30000.0 nM -
CHEMBL1650944 IC50 > 30000.0 nM -