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Assay Detail

CHEMBL1663324

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Binding
Inhibition of PARP1 by chemiluminescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Poly [ADP-ribose] polymerase 1 (CHEMBL3105)
Type SINGLE PROTEIN
Organism Homo sapiens

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 6 6.59 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1652712 1 7.22
CHEMBL1652713 1 6.40
CHEMBL1652711 1 6.16
CHEMBL1652714 1 -
CHEMBL1652715 1 -
CHEMBL1652716 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1652712 IC50 = 60.0 nM 7.22
CHEMBL1652713 IC50 = 400.0 nM 6.40
CHEMBL1652711 IC50 = 700.0 nM 6.16
CHEMBL1652714 IC50 - -
CHEMBL1652715 IC50 - -
CHEMBL1652716 IC50 - -