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Assay Detail

CHEMBL2051671

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

Functional
Antiproliferative activity against human MOLT3 cells expressing FLT3 gene
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MOLT-3
Confidence 1 — Organism
Curated By Autocuration

Target

MOLT-3 (CHEMBL614176)
Type CELL-LINE
Organism Homo sapiens

Publication

An amino-indazole scaffold with spectrum selective kinase inhibition of FLT3, PDGFRα and kit.
Deng X, Zhou W, Weisberg E, Wang J, Zhang J, Sasaki T, Nelson E, Griffin JD, Jänne PA, Gray NS.
Bioorg Med Chem Lett (2012) 22 : 4579 -4584
PubMed 22727638 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 7.23 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2048736 1 8.70
CHEMBL2048845 1 8.70
CHEMBL2048742 1 8.40
CHEMBL2048729 1 8.30
CHEMBL2048735 1 8.30
CHEMBL2048741 1 7.48
CHEMBL2048739 1 7.46
CHEMBL2048730 1 6.49
CHEMBL2048737 1 6.25
CHEMBL2048731 1 5.77
CHEMBL2048738 1 5.46
CHEMBL2048734 1 5.43
CHEMBL2048732 1 -
CHEMBL2048733 1 -
CHEMBL2048740 1 -
CHEMBL2048743 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2048736 EC50 = 2.0 nM 8.70
CHEMBL2048845 EC50 = 2.0 nM 8.70
CHEMBL2048742 EC50 = 4.0 nM 8.40
CHEMBL2048729 EC50 = 5.0 nM 8.30
CHEMBL2048735 EC50 = 5.0 nM 8.30
CHEMBL2048741 EC50 = 33.0 nM 7.48
CHEMBL2048739 EC50 = 35.0 nM 7.46
CHEMBL2048730 EC50 = 325.0 nM 6.49
CHEMBL2048737 EC50 = 559.0 nM 6.25
CHEMBL2048731 EC50 = 1713.0 nM 5.77
CHEMBL2048738 EC50 = 3426.0 nM 5.46
CHEMBL2048734 EC50 = 3752.0 nM 5.43
CHEMBL2048732 EC50 > 10000.0 nM -
CHEMBL2048733 EC50 > 10000.0 nM -
CHEMBL2048740 EC50 < 1.0 nM -
CHEMBL2048743 EC50 < 1.0 nM -