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Assay Detail

CHEMBL3243053

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

Functional
Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 16 hrs by EdU incorporation assay in presence of 10% human serum
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

SJSA-1 (CHEMBL2366298)
Type CELL-LINE
Organism Homo sapiens

Publication

Selective and potent morpholinone inhibitors of the MDM2-p53 protein-protein interaction.
Gonzalez AZ, Eksterowicz J, Bartberger MD, Beck HP, Canon J, Chen A, Chow D, Duquette J, Fox BM, Fu J, Huang X, Houze JB, Jin L, Li Y, Li Z, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, McMinn DL, Oliner JD, Osgood T, Rew Y, Saiki AY, Shaffer P, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Olson SH, Medina JC, Sun D.
J Med Chem (2014) 57 : 2472 -2488
PubMed 24548297 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.05 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3125527 1 8.49
CHEMBL3233140 1 7.60
CHEMBL3233141 1 7.50
CHEMBL3233126 1 7.48
CHEMBL3233137 1 7.48
CHEMBL3233123 1 7.46
CHEMBL3233125 1 7.43
CHEMBL3233130 1 7.43
CHEMBL3233122 1 7.27
CHEMBL3233127 1 7.24
CHEMBL3233138 1 7.17
CHEMBL3233124 1 6.99
CHEMBL3233139 1 6.92
CHEMBL3233136 1 6.89
CHEMBL3233129 1 6.82
CHEMBL3233134 1 6.71
CHEMBL3233131 1 6.70
CHEMBL3233133 1 6.50
CHEMBL3233132 1 6.38
CHEMBL3233121 1 6.30
CHEMBL3233135 1 6.19
CHEMBL3233128 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3125527 IC50 = 3.2 nM 8.49
CHEMBL3233140 IC50 = 25.0 nM 7.60
CHEMBL3233141 IC50 = 32.0 nM 7.50
CHEMBL3233126 IC50 = 33.0 nM 7.48
CHEMBL3233137 IC50 = 33.0 nM 7.48
CHEMBL3233123 IC50 = 35.0 nM 7.46
CHEMBL3233125 IC50 = 37.0 nM 7.43
CHEMBL3233130 IC50 = 37.0 nM 7.43
CHEMBL3233122 IC50 = 54.0 nM 7.27
CHEMBL3233127 IC50 = 58.0 nM 7.24
CHEMBL3233138 IC50 = 67.0 nM 7.17
CHEMBL3233124 IC50 = 103.0 nM 6.99
CHEMBL3233139 IC50 = 120.0 nM 6.92
CHEMBL3233136 IC50 = 129.0 nM 6.89
CHEMBL3233129 IC50 = 150.0 nM 6.82
CHEMBL3233134 IC50 = 195.0 nM 6.71
CHEMBL3233131 IC50 = 198.0 nM 6.70
CHEMBL3233133 IC50 = 315.0 nM 6.50
CHEMBL3233132 IC50 = 421.0 nM 6.38
CHEMBL3233121 IC50 = 500.0 nM 6.30
CHEMBL3233135 IC50 = 641.0 nM 6.19
CHEMBL3233128 IC50 = 800.0 nM 6.10