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Assay Detail

CHEMBL1832182

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Anticancer activity against P-gp overexpressing human NCI/ADR-RES cells after 96 hrs by SRB assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI/ADR-RES
Confidence 1 — Organism
Curated By Autocuration

Target

NCI/ADR-RES (CHEMBL613829)
Type CELL-LINE
Organism Homo sapiens

Publication

Design, synthesis, and SAR studies of 4-substituted methoxylbenzoyl-aryl-thiazoles analogues as potent and orally bioavailable anticancer agents.
Lu Y, Li CM, Wang Z, Chen J, Mohler ML, Li W, Dalton JT, Miller DD.
J Med Chem (2011) 54 : 4678 -4693
PubMed 21557538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.29 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1830231 1 8.40
CHEMBL1830233 1 7.96
CHEMBL1830203 1 7.89
CHEMBL459773 1 7.89
CHEMBL1830219 1 7.85
CHEMBL1830241 1 7.68
CHEMBL1830237 1 7.60
CHEMBL1830198 1 7.57
CHEMBL159 VINBLASTINE 4.0 1 6.24
CHEMBL107 COLCHICINE 4.0 1 5.95
CHEMBL428647 PACLITAXEL 4.0 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1830231 IC50 = 4.0 nM 8.40
CHEMBL1830233 IC50 = 11.0 nM 7.96
CHEMBL1830203 IC50 = 13.0 nM 7.89
CHEMBL459773 IC50 = 13.0 nM 7.89
CHEMBL1830219 IC50 = 14.0 nM 7.85
CHEMBL1830241 IC50 = 21.0 nM 7.68
CHEMBL1830237 IC50 = 25.0 nM 7.60
CHEMBL1830198 IC50 = 27.0 nM 7.57
CHEMBL159 VINBLASTINE IC50 = 582.0 nM 6.24
CHEMBL107 COLCHICINE IC50 = 1113.0 nM 5.95
CHEMBL428647 PACLITAXEL IC50 = 6263.0 nM 5.20