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Assay Detail

CHEMBL1804237

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

Binding
Inhibition of human recombinant CDK5/p25 using Histone H1 and [gamma32]-ATP after 30 mins by scintillation counting
36
Total Activities
36
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, protein kinase inhibitory potencies, and in vitro antiproliferative activities of meridianin derivatives.
Giraud F, Alves G, Debiton E, Nauton L, Théry V, Durieu E, Ferandin Y, Lozach O, Meijer L, Anizon F, Pereira E, Moreau P.
J Med Chem (2011) 54 : 4474 -4489
PubMed 21623630 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 5.52 6.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1802410 1 6.18
CHEMBL1802966 1 6.17
CHEMBL44541 MERIDIANIN C 1 5.92
CHEMBL46440 MERIDIANIN D 1 5.92
CHEMBL1802406 1 5.85
CHEMBL1802404 1 5.80
CHEMBL1802403 1 5.80
CHEMBL1802965 1 5.75
CHEMBL1802967 1 5.68
CHEMBL1802963 1 5.51
CHEMBL1802392 1 5.33
CHEMBL48082 1 5.30
CHEMBL1802396 1 5.22
CHEMBL1802409 1 5.21
CHEMBL1802401 1 5.20
CHEMBL1802389 1 5.17
CHEMBL1802968 1 5.16
CHEMBL1802397 1 5.12
CHEMBL1802391 1 5.12
CHEMBL1802962 1 5.00
CHEMBL1802393 1 -
CHEMBL1802390 1 -
CHEMBL1802394 1 -
CHEMBL1802972 1 -
CHEMBL1802971 1 -
CHEMBL1802970 1 -
CHEMBL1802969 1 -
CHEMBL1802395 1 -
CHEMBL1802398 1 -
CHEMBL1802399 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1802410 IC50 = 660.0 nM 6.18
CHEMBL1802966 IC50 = 680.0 nM 6.17
CHEMBL44541 MERIDIANIN C IC50 = 1200.0 nM 5.92
CHEMBL46440 MERIDIANIN D IC50 = 1200.0 nM 5.92
CHEMBL1802406 IC50 = 1400.0 nM 5.85
CHEMBL1802404 IC50 = 1600.0 nM 5.80
CHEMBL1802403 IC50 = 1600.0 nM 5.80
CHEMBL1802965 IC50 = 1800.0 nM 5.75
CHEMBL1802967 IC50 = 2100.0 nM 5.68
CHEMBL1802963 IC50 = 3100.0 nM 5.51
CHEMBL1802392 IC50 = 4700.0 nM 5.33
CHEMBL48082 IC50 = 5000.0 nM 5.30
CHEMBL1802396 IC50 = 6000.0 nM 5.22
CHEMBL1802409 IC50 = 6200.0 nM 5.21
CHEMBL1802401 IC50 = 6300.0 nM 5.20
CHEMBL1802389 IC50 = 6800.0 nM 5.17
CHEMBL1802968 IC50 = 7000.0 nM 5.16
CHEMBL1802391 IC50 = 7500.0 nM 5.12
CHEMBL1802397 IC50 = 7600.0 nM 5.12
CHEMBL1802962 IC50 = 10000.0 nM 5.00
CHEMBL1802408 IC50 > 10000.0 nM -
CHEMBL1802407 IC50 > 10000.0 nM -
CHEMBL1802405 IC50 > 10000.0 nM -
CHEMBL1802402 IC50 > 10000.0 nM -
CHEMBL1802964 IC50 > 10000.0 nM -
CHEMBL1802400 IC50 > 10000.0 nM -
CHEMBL1802399 IC50 > 10000.0 nM -
CHEMBL1802398 IC50 > 10000.0 nM -
CHEMBL1802395 IC50 > 10000.0 nM -
CHEMBL1802969 IC50 > 10000.0 nM -
CHEMBL1802970 IC50 > 10000.0 nM -
CHEMBL1802971 IC50 > 10000.0 nM -
CHEMBL1802972 IC50 > 10000.0 nM -
CHEMBL1802394 IC50 > 10000.0 nM -
CHEMBL1802390 IC50 > 10000.0 nM -
CHEMBL1802393 IC50 > 10000.0 nM -