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Assay Detail

CHEMBL4118532

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Functional
Antiproliferative activity against human SW620 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SW-620
Confidence 1 — Organism
Curated By Intermediate

Target

SW-620 (CHEMBL612262)
Type CELL-LINE
Organism Homo sapiens

Publication

Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors.
Tan L, Gurbani D, Weisberg EL, Jones DS, Rao S, Singer WD, Bernard FM, Mowafy S, Jenney A, Du G, Nonami A, Griffin JD, Lauffenburger DA, Westover KD, Sorger PK, Gray NS.
Bioorg Med Chem (2017) 25 : 1320 -1328
PubMed 28038940 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.43 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1614701 SELUMETINIB 4.0 1 7.82
CHEMBL3883384 1 7.17
CHEMBL3884293 1 6.61
CHEMBL3884839 1 6.30
CHEMBL3590106 ULIXERTINIB 2.0 1 6.30
CHEMBL3884614 1 6.15
CHEMBL3884960 1 6.12
CHEMBL4127488 1 5.78
CHEMBL1077979 1 5.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1614701 SELUMETINIB IC50 = 15.0 nM 7.82
CHEMBL3883384 IC50 = 67.0 nM 7.17
CHEMBL3884293 IC50 = 247.0 nM 6.61
CHEMBL3884839 IC50 = 506.0 nM 6.30
CHEMBL3590106 ULIXERTINIB IC50 = 499.0 nM 6.30
CHEMBL3884614 IC50 = 707.0 nM 6.15
CHEMBL3884960 IC50 = 767.0 nM 6.12
CHEMBL4127488 IC50 = 1650.0 nM 5.78
CHEMBL1077979 IC50 = 2540.0 nM 5.59