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Assay Detail

CHEMBL832404

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Binding
Inhibition of Cyclin-dependent kinase 4-cyclin D1
99
Total Activities
99
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 biological evaluation of 1-aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of cyclin-dependent kinases.
Markwalder JA, Arnone MR, Benfield PA, Boisclair M, Burton CR, Chang CH, Cox SS, Czerniak PM, Dean CL, Doleniak D, Grafstrom R, Harrison BA, Kaltenbach RF, Nugiel DA, Rossi KA, Sherk SR, Sisk LM, Stouten P, Trainor GL, Worland P, Seitz SP.
J Med Chem (2004) 47 : 5894 -5911
PubMed 15537345 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 99 5.38 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL187984 1 7.70
CHEMBL425181 1 7.40
CHEMBL363174 1 7.30
CHEMBL187522 1 7.22
CHEMBL187816 1 7.10
CHEMBL418203 1 7.05
CHEMBL364001 1 6.80
CHEMBL536272 1 6.34
CHEMBL1790020 1 6.23
CHEMBL363172 1 6.03
CHEMBL365144 1 5.96
CHEMBL365713 1 5.89
CHEMBL188587 1 5.89
CHEMBL433590 1 5.77
CHEMBL188650 1 5.70
CHEMBL366209 1 5.68
CHEMBL370283 1 5.68
CHEMBL186157 1 5.66
CHEMBL364435 1 5.62
CHEMBL363679 1 5.57
CHEMBL190636 1 5.54
CHEMBL187433 1 5.54
CHEMBL190317 1 5.54
CHEMBL362075 1 5.52
CHEMBL188863 1 5.52
CHEMBL187511 1 5.51
CHEMBL373298 1 5.46
CHEMBL188102 1 5.44
CHEMBL187353 1 5.37
CHEMBL191312 1 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL187984 IC50 = 20.0 nM 7.70
CHEMBL425181 IC50 = 40.0 nM 7.40
CHEMBL363174 IC50 = 50.0 nM 7.30
CHEMBL187522 IC50 = 60.0 nM 7.22
CHEMBL187816 IC50 = 80.0 nM 7.10
CHEMBL418203 IC50 = 90.0 nM 7.05
CHEMBL364001 IC50 = 160.0 nM 6.80
CHEMBL536272 IC50 = 460.0 nM 6.34
CHEMBL1790020 IC50 = 590.0 nM 6.23
CHEMBL363172 IC50 = 940.0 nM 6.03
CHEMBL365144 IC50 = 1100.0 nM 5.96
CHEMBL365713 IC50 = 1300.0 nM 5.89
CHEMBL188587 IC50 = 1300.0 nM 5.89
CHEMBL433590 IC50 = 1700.0 nM 5.77
CHEMBL188650 IC50 = 2000.0 nM 5.70
CHEMBL366209 IC50 = 2100.0 nM 5.68
CHEMBL370283 IC50 = 2100.0 nM 5.68
CHEMBL186157 IC50 = 2200.0 nM 5.66
CHEMBL364435 IC50 = 2400.0 nM 5.62
CHEMBL363679 IC50 = 2700.0 nM 5.57
CHEMBL190636 IC50 = 2900.0 nM 5.54
CHEMBL187433 IC50 = 2900.0 nM 5.54
CHEMBL190317 IC50 = 2900.0 nM 5.54
CHEMBL362075 IC50 = 3000.0 nM 5.52
CHEMBL188863 IC50 = 3000.0 nM 5.52
CHEMBL187511 IC50 = 3100.0 nM 5.51
CHEMBL373298 IC50 = 3500.0 nM 5.46
CHEMBL188102 IC50 = 3600.0 nM 5.44
CHEMBL187353 IC50 = 4300.0 nM 5.37
CHEMBL191312 IC50 = 4500.0 nM 5.35
CHEMBL433959 IC50 = 5000.0 nM 5.30
CHEMBL189333 IC50 = 5300.0 nM 5.28
CHEMBL424810 IC50 = 5700.0 nM 5.24
CHEMBL187708 IC50 = 6500.0 nM 5.19
CHEMBL362121 IC50 = 6600.0 nM 5.18
CHEMBL189332 IC50 = 6800.0 nM 5.17
CHEMBL187762 IC50 = 7000.0 nM 5.16
CHEMBL363715 IC50 = 7100.0 nM 5.15
CHEMBL363689 IC50 = 8000.0 nM 5.10
CHEMBL187949 IC50 = 9100.0 nM 5.04
CHEMBL190091 IC50 = 9700.0 nM 5.01
CHEMBL187352 IC50 = 10000.0 nM 5.00
CHEMBL188812 IC50 = 10000.0 nM 5.00
CHEMBL190323 IC50 = 11000.0 nM 4.96
CHEMBL189711 IC50 = 11000.0 nM 4.96
CHEMBL188441 IC50 = 12000.0 nM 4.92
CHEMBL190738 IC50 = 13000.0 nM 4.89
CHEMBL187983 IC50 = 15000.0 nM 4.82
CHEMBL435693 IC50 = 15000.0 nM 4.82
CHEMBL187351 IC50 = 19000.0 nM 4.72