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Assay Detail

CHEMBL2155333

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

Binding
Inhibition of human recombinant GST-tagged CDK5/p25 expressed in Escherichia coli using histone H1 as substrate and [gamma32P]ATP after 30 mins by scintillation counting
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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

Synthesis and biological evaluation of N-arylbenzo[b]thieno[3,2-d]pyrimidin-4-amines and their pyrido and pyrazino analogues as Ser/Thr kinase inhibitors.
Loidreau Y, Marchand P, Dubouilh-Benard C, Nourrisson MR, Duflos M, Lozach O, Loaëc N, Meijer L, Besson T.
Eur J Med Chem (2012) 58 : 171 -183
PubMed 23124214 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 5.28 5.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1836358 1 5.28
CHEMBL2153545 1 -
CHEMBL2153521 1 -
CHEMBL2153520 1 -
CHEMBL2153519 1 -
CHEMBL2153518 1 -
CHEMBL2153411 1 -
CHEMBL2153412 1 -
CHEMBL2153515 1 -
CHEMBL2153516 1 -
CHEMBL2153522 1 -
CHEMBL2153550 1 -
CHEMBL2153549 1 -
CHEMBL2153548 1 -
CHEMBL2153547 1 -
CHEMBL2153546 1 -
CHEMBL2153544 1 -
CHEMBL2153543 1 -
CHEMBL2153531 1 -
CHEMBL2153541 1 -
CHEMBL2153540 1 -
CHEMBL2153539 1 -
CHEMBL2153538 1 -
CHEMBL2153537 1 -
CHEMBL2153536 1 -
CHEMBL2153535 1 -
CHEMBL2153534 1 -
CHEMBL2153533 1 -
CHEMBL2153532 1 -
CHEMBL2153542 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1836358 IC50 = 5200.0 nM 5.28
CHEMBL457313 IC50 > 10000.0 nM -
CHEMBL2153522 IC50 > 10000.0 nM -
CHEMBL2153516 IC50 > 10000.0 nM -
CHEMBL2153515 IC50 > 10000.0 nM -
CHEMBL2153412 IC50 > 10000.0 nM -
CHEMBL2153411 IC50 > 10000.0 nM -
CHEMBL2153518 IC50 > 10000.0 nM -
CHEMBL2153519 IC50 > 10000.0 nM -
CHEMBL2153520 IC50 > 10000.0 nM -
CHEMBL2153521 IC50 > 10000.0 nM -
CHEMBL2153550 IC50 > 10000.0 nM -
CHEMBL2153517 IC50 > 10000.0 nM -
CHEMBL2153523 IC50 > 10000.0 nM -
CHEMBL2153524 IC50 > 10000.0 nM -
CHEMBL2153525 IC50 > 10000.0 nM -
CHEMBL2153526 IC50 > 10000.0 nM -
CHEMBL2153527 IC50 > 10000.0 nM -
CHEMBL2153528 IC50 > 10000.0 nM -
CHEMBL2153529 IC50 > 10000.0 nM -
CHEMBL2153530 IC50 > 10000.0 nM -
CHEMBL2153540 IC50 > 10000.0 nM -
CHEMBL2153542 IC50 > 10000.0 nM -
CHEMBL2153532 IC50 > 10000.0 nM -
CHEMBL2153533 IC50 > 10000.0 nM -
CHEMBL2153534 IC50 > 10000.0 nM -
CHEMBL2153535 IC50 > 10000.0 nM -
CHEMBL2153536 IC50 > 10000.0 nM -
CHEMBL2153537 IC50 > 10000.0 nM -
CHEMBL2153538 IC50 > 10000.0 nM -
CHEMBL2153539 IC50 > 10000.0 nM -
CHEMBL2153549 IC50 > 10000.0 nM -
CHEMBL2153541 IC50 > 10000.0 nM -
CHEMBL2153531 IC50 > 10000.0 nM -
CHEMBL2153543 IC50 > 10000.0 nM -
CHEMBL2153544 IC50 > 10000.0 nM -
CHEMBL2153545 IC50 > 10000.0 nM -
CHEMBL2153546 IC50 > 10000.0 nM -
CHEMBL2153547 IC50 > 10000.0 nM -
CHEMBL2153548 IC50 > 10000.0 nM -