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Assay Detail

CHEMBL1775381

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Functional
Growth inhibition of human GIST882 cells expressing c-Kit after 96 hrs by SRB assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type GIST882
Confidence 1 — Organism
Curated By Autocuration

Publication

Targeting the c-Kit Promoter G-quadruplexes with 6-Substituted Indenoisoquinolines.
Bejugam M, Gunaratnam M, Müller S, Sanders DA, Sewitz S, Fletcher JA, Neidle S, Balasubramanian S.
ACS Med Chem Lett (2010) 1 : 306 -310
PubMed 24900212 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.19 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1642 IMATINIB MESYLATE 4.0 1 5.77
CHEMBL1773218 1 5.39
CHEMBL1773217 1 5.30
CHEMBL1773219 1 4.86
CHEMBL1773221 1 4.64
CHEMBL1773220 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1642 IMATINIB MESYLATE IC50 = 1700.0 nM 5.77
CHEMBL1773218 IC50 = 4100.0 nM 5.39
CHEMBL1773217 IC50 = 5000.0 nM 5.30
CHEMBL1773219 IC50 = 13900.0 nM 4.86
CHEMBL1773221 IC50 = 23000.0 nM 4.64
CHEMBL1773220 IC50 > 50000.0 nM -