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Assay Detail

CHEMBL5712033

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Functional
Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell viability incubated for 5 days by celltiter-glo assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type ZR-75-1
Confidence 1 — Organism
Curated By Autocuration

Target

ZR-75-1 (CHEMBL614393)
Type CELL-LINE
Organism Homo sapiens

Publication

Structural and chemical insights into the covalent-allosteric inhibition of the protein kinase Akt.
Uhlenbrock N, Smith S, Weisner J, Landel I, Lindemann M, Le TA, Hardick J, Gontla R, Scheinpflug R, Czodrowski P, Janning P, Depta L, Quambusch L, Müller MP, Engels B, Rauh D.
Chem Sci (2019) 10 : 3573 -3585
PubMed 30996949 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 7.38 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5712048 1 8.70
CHEMBL5712063 1 8.70
CHEMBL4795065 Borussertib 1 8.30
CHEMBL5712046 1 8.00
CHEMBL5712042 1 7.96
CHEMBL5712045 1 7.66
CHEMBL5712066 1 7.48
CHEMBL5712049 1 7.41
CHEMBL1079175 MK-2206 2.0 1 7.20
CHEMBL5712044 1 7.14
CHEMBL53463 DOXORUBICIN 4.0 1 7.00
CHEMBL5712058 1 6.94
CHEMBL5712055 1 6.82
CHEMBL2325741 CAPIVASERTIB 4.0 1 6.72
CHEMBL2177390 IPATASERTIB 3.0 1 6.66
CHEMBL5712059 1 6.42
CHEMBL5712061 1 6.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5712048 EC50 = 2.0 nM 8.70
CHEMBL5712063 EC50 = 2.0 nM 8.70
CHEMBL4795065 Borussertib EC50 = 5.0 nM 8.30
CHEMBL5712046 EC50 = 10.0 nM 8.00
CHEMBL5712042 EC50 = 11.0 nM 7.96
CHEMBL5712045 EC50 = 22.0 nM 7.66
CHEMBL5712066 EC50 = 33.0 nM 7.48
CHEMBL5712049 EC50 = 39.0 nM 7.41
CHEMBL1079175 MK-2206 EC50 = 63.0 nM 7.20
CHEMBL5712044 EC50 = 73.0 nM 7.14
CHEMBL53463 DOXORUBICIN EC50 = 100.0 nM 7.00
CHEMBL5712058 EC50 = 116.0 nM 6.94
CHEMBL5712055 EC50 = 151.0 nM 6.82
CHEMBL2325741 CAPIVASERTIB EC50 = 191.0 nM 6.72
CHEMBL2177390 IPATASERTIB EC50 = 219.0 nM 6.66
CHEMBL5712059 EC50 = 384.0 nM 6.42
CHEMBL5712061 EC50 = 427.0 nM 6.37