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Assay Detail

CHEMBL2091391

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Functional
Antiproliferative activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type U2OS
Confidence 1 — Organism
Curated By Autocuration

Target

U2OS (CHEMBL615023)
Type CELL-LINE
Organism Homo sapiens

Publication

Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors.
Guo Z, Zhuang C, Zhu L, Zhang Y, Yao J, Dong G, Wang S, Liu Y, Chen H, Sheng C, Miao Z, Zhang W.
Eur J Med Chem (2012) 56 : 10 -16
PubMed 22940704 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 4.75 5.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2089153 1 5.58
CHEMBL2089151 1 5.46
CHEMBL2089203 1 5.25
CHEMBL2089201 1 5.14
CHEMBL2089208 1 5.12
CHEMBL2089204 1 4.93
CHEMBL2089152 1 4.92
CHEMBL2089149 1 4.92
CHEMBL1909836 1 4.80
CHEMBL191334 NUTLIN-3 1 4.71
CHEMBL2089211 1 4.56
CHEMBL2089206 1 4.56
CHEMBL2089209 1 4.55
CHEMBL2089207 1 4.49
CHEMBL2089320 1 4.47
CHEMBL2089205 1 4.45
CHEMBL2089210 1 4.45
CHEMBL2089200 1 4.35
CHEMBL2089321 1 4.17
CHEMBL2089150 1 4.05
CHEMBL2089202 1 -
CHEMBL2089322 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2089153 IC50 = 2610.0 nM 5.58
CHEMBL2089151 IC50 = 3500.0 nM 5.46
CHEMBL2089203 IC50 = 5690.0 nM 5.25
CHEMBL2089201 IC50 = 7230.0 nM 5.14
CHEMBL2089208 IC50 = 7530.0 nM 5.12
CHEMBL2089204 IC50 = 11800.0 nM 4.93
CHEMBL2089152 IC50 = 12000.0 nM 4.92
CHEMBL2089149 IC50 = 12100.0 nM 4.92
CHEMBL1909836 IC50 = 15900.0 nM 4.80
CHEMBL191334 NUTLIN-3 IC50 = 19600.0 nM 4.71
CHEMBL2089211 IC50 = 27400.0 nM 4.56
CHEMBL2089206 IC50 = 27800.0 nM 4.56
CHEMBL2089209 IC50 = 28000.0 nM 4.55
CHEMBL2089207 IC50 = 32700.0 nM 4.49
CHEMBL2089320 IC50 = 33900.0 nM 4.47
CHEMBL2089205 IC50 = 35300.0 nM 4.45
CHEMBL2089210 IC50 = 35700.0 nM 4.45
CHEMBL2089200 IC50 = 44300.0 nM 4.35
CHEMBL2089321 IC50 = 67600.0 nM 4.17
CHEMBL2089150 IC50 = 88500.0 nM 4.05
CHEMBL2089202 IC50 > 100000.0 nM -
CHEMBL2089322 IC50 > 100000.0 nM -