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Assay Detail

CHEMBL5229242

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

Binding
Binding affinity to Mycobacterium tuberculosis partial length PknB (M1 to G279 residues) expressed in mammalian expression system by KdELECT kinase assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mycobacterium tuberculosis
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase PknB (CHEMBL1908385)
Type SINGLE PROTEIN
Organism Mycobacterium tuberculosis

Publication

Engineering Selectivity for Reduced Toxicity of Bacterial Kinase Inhibitors Using Structure-Guided Medicinal Chemistry.
Wlodarchak N, Feltenberger JB, Ye Z, Beczkiewicz J, Procknow R, Yan G, King TM, Golden JE, Striker R.
ACS Med Chem Lett (2021) 12 : 228 -235
PubMed 35035774 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 7.15 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5282194 1 7.72
CHEMBL468963 GW779439X 1 7.58
CHEMBL5283441 1 7.33
CHEMBL5283041 1 6.75
CHEMBL5283475 1 6.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5282194 Kd = 19.0 nM 7.72
CHEMBL468963 GW779439X Kd = 26.0 nM 7.58
CHEMBL5283441 Kd = 47.0 nM 7.33
CHEMBL5283041 Kd = 180.0 nM 6.75
CHEMBL5283475 Kd = 430.0 nM 6.37