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Assay Detail

CHEMBL5100012

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

Binding
Inhibition of CK1alpha (unknown origin)
4
Total Activities
4
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

Casein kinase I isoform alpha (CHEMBL2793)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Phenotypic Discovery of Triazolo[1,5-<i>c</i>]quinazolines as a First-In-Class Bone Morphogenetic Protein Amplifier Chemotype.
Wesseler F, Lohmann S, Riege D, Halver J, Roth A, Pichlo C, Weber S, Takamiya M, Müller E, Ketzel J, Flegel J, Gihring A, Rastegar S, Bertrand J, Baumann U, Knippschild U, Peifer C, Sievers S, Waldmann H, Schade D.
J Med Chem (2022) 65 : 15263 -15281
PubMed 36346705 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.88 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5186013 1 6.66
CHEMBL16687 CGS-15943 1 6.09
CHEMBL5182545 1 5.54
CHEMBL268550 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5186013 IC50 = 220.0 nM 6.66
CHEMBL16687 CGS-15943 IC50 = 820.0 nM 6.09
CHEMBL5182545 IC50 = 2920.0 nM 5.54
CHEMBL268550 IC50 = 6180.0 nM 5.21