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Assay Detail

CHEMBL666303

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Binding
Binding affinity for Cyclin-dependent kinase 4-cyclin D1
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Cyclin-dependent kinase 4/cyclin D1 (CHEMBL1907601)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3.
Yue EW, DiMeo SV, Higley CA, Markwalder JA, Burton CR, Benfield PA, Grafstrom RH, Cox S, Muckelbauer JK, Smallwood AM, Chen H, Chang CH, Trainor GL, Seitz SP.
Bioorg Med Chem Lett (2004) 14 : 343 -346
PubMed 14698155 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 7.53 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL115706 1 8.52
CHEMBL334285 1 8.40
CHEMBL326961 1 8.40
CHEMBL117939 1 8.30
CHEMBL116619 1 8.30
CHEMBL114053 1 8.15
CHEMBL116934 1 8.15
CHEMBL324612 1 8.10
CHEMBL117473 1 8.00
CHEMBL323813 1 7.92
CHEMBL117647 1 7.89
CHEMBL113867 1 7.82
CHEMBL332712 1 7.77
CHEMBL116646 1 7.68
CHEMBL116331 1 7.66
CHEMBL326828 1 7.66
CHEMBL323908 1 7.64
CHEMBL411432 1 7.64
CHEMBL119106 1 7.52
CHEMBL117259 1 7.52
CHEMBL116670 1 7.46
CHEMBL325023 1 7.34
CHEMBL117712 1 7.09
CHEMBL325453 1 7.08
CHEMBL118027 1 7.07
CHEMBL116582 1 7.05
CHEMBL116510 1 6.97
CHEMBL273619 1 6.90
CHEMBL119493 1 6.82
CHEMBL117866 1 6.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL115706 IC50 = 3.0 nM 8.52
CHEMBL334285 IC50 = 4.0 nM 8.40
CHEMBL326961 IC50 = 4.0 nM 8.40
CHEMBL117939 IC50 = 5.0 nM 8.30
CHEMBL116619 IC50 = 5.0 nM 8.30
CHEMBL114053 IC50 = 7.0 nM 8.15
CHEMBL116934 IC50 = 7.0 nM 8.15
CHEMBL324612 IC50 = 8.0 nM 8.10
CHEMBL117473 IC50 = 10.0 nM 8.00
CHEMBL323813 IC50 = 12.0 nM 7.92
CHEMBL117647 IC50 = 13.0 nM 7.89
CHEMBL113867 IC50 = 15.0 nM 7.82
CHEMBL332712 IC50 = 17.0 nM 7.77
CHEMBL116646 IC50 = 21.0 nM 7.68
CHEMBL326828 IC50 = 22.0 nM 7.66
CHEMBL116331 IC50 = 22.0 nM 7.66
CHEMBL411432 IC50 = 23.0 nM 7.64
CHEMBL323908 IC50 = 23.0 nM 7.64
CHEMBL119106 IC50 = 30.0 nM 7.52
CHEMBL117259 IC50 = 30.0 nM 7.52
CHEMBL116670 IC50 = 35.0 nM 7.46
CHEMBL325023 IC50 = 46.0 nM 7.34
CHEMBL117712 IC50 = 81.0 nM 7.09
CHEMBL325453 IC50 = 84.0 nM 7.08
CHEMBL118027 IC50 = 86.0 nM 7.07
CHEMBL116582 IC50 = 90.0 nM 7.05
CHEMBL116510 IC50 = 107.0 nM 6.97
CHEMBL273619 IC50 = 125.0 nM 6.90
CHEMBL119493 IC50 = 150.0 nM 6.82
CHEMBL117866 IC50 = 185.0 nM 6.73
CHEMBL117593 IC50 = 340.0 nM 6.47
CHEMBL116647 IC50 = 515.0 nM 6.29
CHEMBL116081 IC50 = 635.0 nM 6.20
CHEMBL114464 IC50 > 370.0 nM -