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Assay Detail

CHEMBL3364005

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Functional
Antiproliferative activity against wild-type p53 expressing human HCT116 cells assessed as inhibition of cell proliferation by MTT assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT-116
Confidence 1 — Organism
Curated By Autocuration

Publication

Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy.
Zhang Z, Ding Q, Liu JJ, Zhang J, Jiang N, Chu XJ, Bartkovitz D, Luk KC, Janson C, Tovar C, Filipovic ZM, Higgins B, Glenn K, Packman K, Vassilev LT, Graves B.
Bioorg Med Chem (2014) 22 : 4001 -4009
PubMed 24997575 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.17 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3310320 1 8.10
CHEMBL3310184 1 8.00
CHEMBL3310188 1 7.70
CHEMBL3310182 1 7.30
CHEMBL3310185 1 7.16
CHEMBL3310186 1 7.10
CHEMBL3310321 1 6.92
CHEMBL3310187 1 6.92
CHEMBL3310319 1 6.75
CHEMBL3310322 1 6.75
CHEMBL3310323 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3310320 IC50 = 8.0 nM 8.10
CHEMBL3310184 IC50 = 10.0 nM 8.00
CHEMBL3310188 IC50 = 20.0 nM 7.70
CHEMBL3310182 IC50 = 50.0 nM 7.30
CHEMBL3310185 IC50 = 70.0 nM 7.16
CHEMBL3310186 IC50 = 80.0 nM 7.10
CHEMBL3310321 IC50 = 120.0 nM 6.92
CHEMBL3310187 IC50 = 120.0 nM 6.92
CHEMBL3310319 IC50 = 180.0 nM 6.75
CHEMBL3310322 IC50 = 180.0 nM 6.75
CHEMBL3310323 IC50 = 670.0 nM 6.17