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Assay Detail

CHEMBL666606

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

Binding
Inhibitory activity against baculovirus expressed Cyclin dependent kinase 4-cyclinD1
22
Total Activities
22
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

Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.
Kim KS, Kimball SD, Misra RN, Rawlins DB, Hunt JT, Xiao HY, Lu S, Qian L, Han WC, Shan W, Mitt T, Cai ZW, Poss MA, Zhu H, Sack JS, Tokarski JS, Chang CY, Pavletich N, Kamath A, Humphreys WG, Marathe P, Bursuker I, Kellar KA, Roongta U, Batorsky R, Mulheron JG, Bol D, Fairchild CR, Lee FY, Webster KR.
J Med Chem (2002) 45 : 3905 -3927
PubMed 12190313 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 5.87 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL126630 1 7.52
CHEMBL300936 1 7.00
CHEMBL428690 ALVOCIDIB 3.0 1 6.82
CHEMBL126997 1 6.41
CHEMBL126328 1 6.19
CHEMBL295136 1 6.16
CHEMBL340794 1 6.05
CHEMBL48796 1 6.02
CHEMBL129471 1 5.97
CHEMBL126993 1 5.97
CHEMBL129396 1 5.96
CHEMBL125401 1 5.65
CHEMBL126908 1 5.52
CHEMBL2111846 1 5.50
CHEMBL263955 1 5.46
CHEMBL125731 1 5.35
CHEMBL420143 1 5.29
CHEMBL340012 1 5.27
CHEMBL339246 1 4.72
CHEMBL127929 1 4.64
CHEMBL126549 1 -
CHEMBL126782 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL126630 IC50 = 30.0 nM 7.52
CHEMBL300936 IC50 = 100.0 nM 7.00
CHEMBL428690 ALVOCIDIB IC50 = 150.0 nM 6.82
CHEMBL126997 IC50 = 390.0 nM 6.41
CHEMBL126328 IC50 = 640.0 nM 6.19
CHEMBL295136 IC50 = 690.0 nM 6.16
CHEMBL340794 IC50 = 900.0 nM 6.05
CHEMBL48796 IC50 = 960.0 nM 6.02
CHEMBL129471 IC50 = 1070.0 nM 5.97
CHEMBL126993 IC50 = 1070.0 nM 5.97
CHEMBL129396 IC50 = 1090.0 nM 5.96
CHEMBL125401 IC50 = 2250.0 nM 5.65
CHEMBL126908 IC50 = 2990.0 nM 5.52
CHEMBL2111846 IC50 = 3130.0 nM 5.50
CHEMBL263955 IC50 = 3480.0 nM 5.46
CHEMBL125731 IC50 = 4510.0 nM 5.35
CHEMBL420143 IC50 = 5160.0 nM 5.29
CHEMBL340012 IC50 = 5380.0 nM 5.27
CHEMBL339246 IC50 = 19060.0 nM 4.72
CHEMBL127929 IC50 = 23030.0 nM 4.64
CHEMBL126549 IC50 > 1000.0 nM -
CHEMBL126782 IC50 > 25000.0 nM -