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Assay Detail

CHEMBL1663322

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

Binding
Inhibition of CK2 assessed as inhibition of [gamma32P]GTP incorporation into substrate by liquid scintillation counting
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer.
Pierre F, Chua PC, O'Brien SE, Siddiqui-Jain A, Bourbon P, Haddach M, Michaux J, Nagasawa J, Schwaebe MK, Stefan E, Vialettes A, Whitten JP, Chen TK, Darjania L, Stansfield R, Anderes K, Bliesath J, Drygin D, Ho C, Omori M, Proffitt C, Streiner N, Trent K, Rice WG, Ryckman DM.
J Med Chem (2011) 54 : 635 -654
PubMed 21174434 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.26 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL289277 EMODIN 1 5.70
CHEMBL375530 DICHLORORIBOBENZIMIDAZOLE 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL289277 EMODIN IC50 = 2000.0 nM 5.70
CHEMBL375530 DICHLORORIBOBENZIMIDAZOLE IC50 = 15000.0 nM 4.82