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Assay Detail

CHEMBL5048671

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

Binding
Inhibition of Nano-Luc fused human full length CDK5/P35 transfected in HEK293 cells incubated for 1 hr by NanoBRET assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 5/CDK5 activator 1 (CHEMBL1907600)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery and Optimization of Highly Selective Inhibitors of CDK5.
Daniels MH, Malojcic G, Clugston SL, Williams B, Coeffet-Le Gal M, Pan-Zhou XR, Venkatachalan S, Harmange JC, Ledeboer M.
J Med Chem (2022) 65 : 3575 -3596
PubMed 35143203 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.80 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5080866 1 9.70
CHEMBL5080566 1 9.00
CHEMBL5088315 1 8.92
CHEMBL5078192 1 8.92
CHEMBL5079342 1 8.43
CHEMBL2103840 DINACICLIB 3.0 1 7.80
CHEMBL5083778 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5080866 IC50 = 0.2 nM 9.70
CHEMBL5080566 IC50 = 1.0 nM 9.00
CHEMBL5088315 IC50 = 1.2 nM 8.92
CHEMBL5078192 IC50 = 1.2 nM 8.92
CHEMBL5079342 IC50 = 3.7 nM 8.43
CHEMBL2103840 DINACICLIB IC50 = 16.0 nM 7.80
CHEMBL5083778 IC50 - -