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Assay Detail

CHEMBL2406217

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

Functional
Cytotoxicity against human HOS cells assessed as growth inhibition after 72 hrs by calcein AM staining-based fluoroscence assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HOS
Confidence 1 — Organism
Curated By Autocuration

Target

HOS (CHEMBL614736)
Type CELL-LINE
Organism Homo sapiens

Publication

A novel series of highly potent 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitors.
Gucký T, Jorda R, Zatloukal M, Bazgier V, Berka K, Řezníčková E, Béres T, Strnad M, Kryštof V.
J Med Chem (2013) 56 : 6234 -6247
PubMed 23829517 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.57 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2402946 1 7.85
CHEMBL2403095 1 7.62
CHEMBL2403096 1 7.50
CHEMBL2403094 1 7.36
CHEMBL2403093 1 7.36
CHEMBL2403097 1 7.05
CHEMBL2403084 1 6.99
CHEMBL2403088 1 6.99
CHEMBL2403087 1 6.92
CHEMBL2403092 1 6.91
CHEMBL2403085 1 6.85
CHEMBL2402954 1 6.82
CHEMBL2402949 1 6.77
CHEMBL2403098 1 6.75
CHEMBL2403090 1 6.69
CHEMBL2403083 1 6.68
CHEMBL2403086 1 6.61
CHEMBL2402952 1 6.54
CHEMBL2403091 1 6.40
CHEMBL2402947 1 6.31
CHEMBL2403099 1 6.25
CHEMBL2402951 1 6.03
CHEMBL2402950 1 6.00
CHEMBL2402945 1 5.94
CHEMBL2402953 1 5.73
CHEMBL2402948 1 5.69
CHEMBL2403089 1 4.67
CHEMBL14762 SELICICLIB 2.0 1 4.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2402946 IC50 = 14.0 nM 7.85
CHEMBL2403095 IC50 = 24.0 nM 7.62
CHEMBL2403096 IC50 = 32.0 nM 7.50
CHEMBL2403094 IC50 = 44.0 nM 7.36
CHEMBL2403093 IC50 = 44.0 nM 7.36
CHEMBL2403097 IC50 = 89.0 nM 7.05
CHEMBL2403084 IC50 = 102.0 nM 6.99
CHEMBL2403088 IC50 = 103.0 nM 6.99
CHEMBL2403087 IC50 = 120.0 nM 6.92
CHEMBL2403092 IC50 = 122.0 nM 6.91
CHEMBL2403085 IC50 = 140.0 nM 6.85
CHEMBL2402954 IC50 = 150.0 nM 6.82
CHEMBL2402949 IC50 = 170.0 nM 6.77
CHEMBL2403098 IC50 = 180.0 nM 6.75
CHEMBL2403090 IC50 = 206.0 nM 6.69
CHEMBL2403083 IC50 = 211.0 nM 6.68
CHEMBL2403086 IC50 = 247.0 nM 6.61
CHEMBL2402952 IC50 = 290.0 nM 6.54
CHEMBL2403091 IC50 = 398.0 nM 6.40
CHEMBL2402947 IC50 = 490.0 nM 6.31
CHEMBL2403099 IC50 = 560.0 nM 6.25
CHEMBL2402951 IC50 = 935.0 nM 6.03
CHEMBL2402950 IC50 = 995.0 nM 6.00
CHEMBL2402945 IC50 = 1160.0 nM 5.94
CHEMBL2402953 IC50 = 1881.0 nM 5.73
CHEMBL2402948 IC50 = 2030.0 nM 5.69
CHEMBL2403089 IC50 = 21410.0 nM 4.67
CHEMBL14762 SELICICLIB IC50 = 24300.0 nM 4.61