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Assay Detail

CHEMBL993952

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

Binding
Inhibition of human recombinant CDK5/p25 expressed in Escherichia coli
6
Total Activities
6
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

Pyrazolo[1,5-a]-1,3,5-triazine as a purine bioisostere: access to potent cyclin-dependent kinase inhibitor (R)-roscovitine analogue.
Popowycz F, Fournet G, Schneider C, Bettayeb K, Ferandin Y, Lamigeon C, Tirado OM, Mateo-Lozano S, Notario V, Colas P, Bernard P, Meijer L, Joseph B.
J Med Chem (2009) 52 : 655 -663
PubMed 19128055 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.91 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL480442 1 7.22
CHEMBL482193 1 7.16
CHEMBL23327 PURVALANOLA 1 7.12
CHEMBL521274 1 6.89
CHEMBL14762 SELICICLIB 2.0 1 6.57
CHEMBL482211 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL480442 IC50 = 60.0 nM 7.22
CHEMBL482193 IC50 = 70.0 nM 7.16
CHEMBL23327 PURVALANOLA IC50 = 75.0 nM 7.12
CHEMBL521274 IC50 = 130.0 nM 6.89
CHEMBL14762 SELICICLIB IC50 = 270.0 nM 6.57
CHEMBL482211 IC50 = 320.0 nM 6.50