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Assay Detail

CHEMBL5167577

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Binding
Binding affinity to human N-terminal His-tagged/ TEV cleavage fused DRAK1 (39 to 369 residues) expressed in Escherichia coli by isothermal titration calorimetry
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

Serine/threonine-protein kinase 17A (CHEMBL4525)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Illuminating the Dark: Highly Selective Inhibition of Serine/Threonine Kinase 17A with Pyrazolo[1,5-<i>a</i>]pyrimidine-Based Macrocycles.
Kurz CG, Preuss F, Tjaden A, Cusack M, Amrhein JA, Chatterjee D, Mathea S, Berger LM, Berger BT, Krämer A, Weller M, Weiss T, Müller S, Knapp S, Hanke T.
J Med Chem (2022) 65 : 7799 -7817
PubMed 35608370 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 7.87 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5191892 1 8.05
CHEMBL5087558 1 7.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5191892 Kd = 9.0 nM 8.05
CHEMBL5087558 Kd = 21.0 nM 7.68