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Assay Detail

CHEMBL1949178

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

Binding
Inhibition of human recombinant CDK5/p25 using [gamma-33P]ATP after 30 mins by scintillation counting
20
Total Activities
20
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 of chromeno[3,4-b]indoles as Lamellarin D analogues: a novel DYRK1A inhibitor class.
Neagoie C, Vedrenne E, Buron F, Mérour JY, Rosca S, Bourg S, Lozach O, Meijer L, Baldeyrou B, Lansiaux A, Routier S.
Eur J Med Chem (2012) 49 : 379 -396
PubMed 22305342 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.33 6.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1947110 1 6.14
CHEMBL1947105 1 5.57
CHEMBL1946917 1 5.38
CHEMBL1946916 1 5.33
CHEMBL1947112 1 5.08
CHEMBL1946918 1 5.00
CHEMBL1947117 1 4.80
CHEMBL1947116 1 -
CHEMBL1947115 1 -
CHEMBL1947114 1 -
CHEMBL1947113 1 -
CHEMBL1947111 1 -
CHEMBL1947109 1 -
CHEMBL1947108 1 -
CHEMBL1947107 1 -
CHEMBL1947106 1 -
CHEMBL1946915 1 -
CHEMBL1946914 1 -
CHEMBL1946913 1 -
CHEMBL1944663 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1947110 IC50 = 720.0 nM 6.14
CHEMBL1947105 IC50 = 2700.0 nM 5.57
CHEMBL1946917 IC50 = 4200.0 nM 5.38
CHEMBL1946916 IC50 = 4700.0 nM 5.33
CHEMBL1947112 IC50 = 8400.0 nM 5.08
CHEMBL1946918 IC50 = 10000.0 nM 5.00
CHEMBL1947117 IC50 = 16000.0 nM 4.80
CHEMBL1947116 IC50 > 10000.0 nM -
CHEMBL1947115 IC50 > 10000.0 nM -
CHEMBL1947114 IC50 > 10000.0 nM -
CHEMBL1947113 IC50 >= 10000.0 nM -
CHEMBL1947111 IC50 > 10000.0 nM -
CHEMBL1947109 IC50 >= 10000.0 nM -
CHEMBL1947108 IC50 > 10000.0 nM -
CHEMBL1947107 IC50 > 10000.0 nM -
CHEMBL1947106 IC50 >= 10000.0 nM -
CHEMBL1946915 IC50 >= 10000.0 nM -
CHEMBL1946914 IC50 > 10000.0 nM -
CHEMBL1946913 IC50 > 10000.0 nM -
CHEMBL1944663 IC50 > 10000.0 nM -