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Assay Detail

CHEMBL820843

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

Binding
Inhibitory activity against CDK4 using recombinant human cyclin D2-CDK4 complex expressed in sf9 cells
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structure-based generation of a new class of potent Cdk4 inhibitors: new de novo design strategy and library design.
Honma T, Hayashi K, Aoyama T, Hashimoto N, Machida T, Fukasawa K, Iwama T, Ikeura C, Ikuta M, Suzuki-Takahashi I, Iwasawa Y, Hayama T, Nishimura S, Morishima H.
J Med Chem (2001) 44 : 4615 -4627
PubMed 11741479 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 5.46 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL143588 1 7.96
CHEMBL344130 1 7.77
CHEMBL143580 1 7.47
CHEMBL141247 1 7.38
CHEMBL140589 1 7.00
CHEMBL342863 1 6.72
CHEMBL143759 1 6.17
CHEMBL143704 1 5.62
CHEMBL140583 1 5.44
CHEMBL140624 1 5.12
CHEMBL141962 1 4.85
CHEMBL341824 PTEROIC ACID 1 4.80
CHEMBL139990 1 4.64
CHEMBL142641 1 4.44
CHEMBL356687 1 4.44
CHEMBL143713 1 4.40
CHEMBL342899 1 4.36
CHEMBL357170 1 4.11
CHEMBL139814 1 4.05
CHEMBL357461 1 4.00
CHEMBL143703 1 4.00
CHEMBL585 TRIAMTERENE 4.0 1 -
CHEMBL140573 1 -
CHEMBL342186 1 -
CHEMBL141987 1 -
CHEMBL140053 1 -
CHEMBL141224 1 -
CHEMBL140574 1 -
CHEMBL142698 1 -
CHEMBL141952 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL143588 IC50 = 11.0 nM 7.96
CHEMBL344130 IC50 = 17.0 nM 7.77
CHEMBL143580 IC50 = 34.0 nM 7.47
CHEMBL141247 IC50 = 42.0 nM 7.38
CHEMBL140589 IC50 = 100.0 nM 7.00
CHEMBL342863 IC50 = 190.0 nM 6.72
CHEMBL143759 IC50 = 670.0 nM 6.17
CHEMBL143704 IC50 = 2400.0 nM 5.62
CHEMBL140583 IC50 = 3600.0 nM 5.44
CHEMBL140624 IC50 = 7600.0 nM 5.12
CHEMBL141962 IC50 = 14000.0 nM 4.85
CHEMBL341824 PTEROIC ACID IC50 = 16000.0 nM 4.80
CHEMBL139990 IC50 = 23000.0 nM 4.64
CHEMBL142641 IC50 = 36000.0 nM 4.44
CHEMBL356687 IC50 = 36000.0 nM 4.44
CHEMBL143713 IC50 = 40000.0 nM 4.40
CHEMBL342899 IC50 = 44000.0 nM 4.36
CHEMBL357170 IC50 = 77000.0 nM 4.11
CHEMBL139814 IC50 = 90000.0 nM 4.05
CHEMBL357461 IC50 = 100000.0 nM 4.00
CHEMBL143703 IC50 = 100000.0 nM 4.00
CHEMBL585 TRIAMTERENE IC50 = 210000.0 nM -
CHEMBL140573 IC50 = 150000.0 nM -
CHEMBL342186 IC50 = 340000.0 nM -
CHEMBL141987 IC50 > 100000.0 nM -
CHEMBL140053 IC50 > 100000.0 nM -
CHEMBL141224 IC50 > 1000000.0 nM -
CHEMBL140574 IC50 = 220000.0 nM -
CHEMBL142698 IC50 = 450000.0 nM -
CHEMBL141952 IC50 = 110000.0 nM -
CHEMBL139989 IC50 = 410000.0 nM -
CHEMBL342003 IC50 = 120000.0 nM -
CHEMBL141159 IC50 = 350000.0 nM -