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Assay Detail

CHEMBL1656783

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

Functional
Cytotoxicity against human NCI-ADR-RES expressing MDR1 cells after 48 to 72 hrs by WAT-1 assay
6
Total Activities
6
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

Publication

Synthesis and pharmacological evaluation of N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a potent antimitotic agent.
Shetty RS, Lee Y, Liu B, Husain A, Joseph RW, Lu Y, Nelson D, Mihelcic J, Chao W, Moffett KK, Schumacher A, Flubacher D, Stojanovic A, Bukhtiyarova M, Williams K, Lee KJ, Ochman AR, Saporito MS, Moore WR, Flynn GA, Dorsey BD, Springman EB, Fujimoto T, Kelly MJ.
J Med Chem (2011) 54 : 179 -200
PubMed 21126027 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.15 6.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20684 ABT-751 2.0 1 6.54
CHEMBL1649644 1 6.52
CHEMBL1649645 1 6.52
CHEMBL1649615 1 6.47
CHEMBL1649648 1 5.96
CHEMBL428647 PACLITAXEL 4.0 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20684 ABT-751 IC50 = 290.0 nM 6.54
CHEMBL1649644 IC50 = 300.0 nM 6.52
CHEMBL1649645 IC50 = 300.0 nM 6.52
CHEMBL1649615 IC50 = 340.0 nM 6.47
CHEMBL1649648 IC50 = 1100.0 nM 5.96
CHEMBL428647 PACLITAXEL IC50 = 13000.0 nM 4.89