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Assay Detail

CHEMBL3404064

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Functional
Antiproliferative activity against human A431 cells after 48 hrs by sulforhodamine B assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A-431
Confidence 1 — Organism
Curated By Autocuration

Target

A-431 (CHEMBL614069)
Type CELL-LINE
Organism Homo sapiens

Publication

The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.
Zhang X, Raghavan S, Ihnat M, Hamel E, Zammiello C, Bastian A, Mooberry SL, Gangjee A.
Bioorg Med Chem (2015) 23 : 2408 -2423
PubMed 25882519 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.54 8.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3403510 1 8.01
CHEMBL3403518 1 7.94
CHEMBL3403509 1 7.77
CHEMBL3403517 1 7.75
CHEMBL3297898 1 7.68
CHEMBL3403513 1 7.42
CHEMBL3403515 1 7.38
CHEMBL3403512 1 7.31
CHEMBL3403514 1 7.13
CHEMBL3403519 1 7.03
CHEMBL3403511 1 -
CHEMBL3403516 1 -
CHEMBL553 ERLOTINIB 4.0 1 -
CHEMBL276711 SEMAXANIB 3.0 1 -
CHEMBL535 SUNITINIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3403510 IC50 = 9.7 nM 8.01
CHEMBL3403518 IC50 = 11.6 nM 7.94
CHEMBL3403509 IC50 = 17.1 nM 7.77
CHEMBL3403517 IC50 = 18.0 nM 7.75
CHEMBL3297898 IC50 = 20.8 nM 7.68
CHEMBL3403513 IC50 = 38.3 nM 7.42
CHEMBL3403515 IC50 = 42.2 nM 7.38
CHEMBL3403512 IC50 = 48.9 nM 7.31
CHEMBL3403514 IC50 = 73.2 nM 7.13
CHEMBL3403519 IC50 = 92.9 nM 7.03
CHEMBL3403511 IC50 > 300.0 nM -
CHEMBL3403516 IC50 > 300.0 nM -
CHEMBL553 ERLOTINIB IC50 - -
CHEMBL276711 SEMAXANIB IC50 - -
CHEMBL535 SUNITINIB IC50 - -