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Assay Detail

CHEMBL2038858

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

Functional
Antiproliferative activity against mouse BA/F3 cells expressing Tel-KDR
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type BaF3
Confidence 1 — Organism
Curated By Autocuration

Publication

Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models.
Albaugh P, Fan Y, Mi Y, Sun F, Adrian F, Li N, Jia Y, Sarkisova Y, Kreusch A, Hood T, Lu M, Liu G, Huang S, Liu Z, Loren J, Tuntland T, Karanewsky DS, Seidel HM, Molteni V.
ACS Med Chem Lett (2012) 3 : 140 -145
PubMed 24900443 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.03 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2037215 1 6.70
CHEMBL2037221 1 6.64
CHEMBL2037208 1 6.30
CHEMBL2037209 1 6.30
CHEMBL2037211 1 6.30
CHEMBL2037224 1 6.28
CHEMBL2037194 1 6.22
CHEMBL2037218 1 6.22
CHEMBL2037213 1 6.21
CHEMBL2037212 1 6.16
CHEMBL2037193 1 6.00
CHEMBL2037222 1 5.89
CHEMBL2037220 1 5.82
CHEMBL2037217 1 5.66
CHEMBL2037210 1 5.55
CHEMBL2037226 1 5.52
CHEMBL2037225 1 5.48
CHEMBL2037214 1 5.31
CHEMBL2037216 1 -
CHEMBL2037219 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2037215 IC50 = 200.0 nM 6.70
CHEMBL2037221 IC50 = 230.0 nM 6.64
CHEMBL2037208 IC50 = 500.0 nM 6.30
CHEMBL2037209 IC50 = 500.0 nM 6.30
CHEMBL2037211 IC50 = 500.0 nM 6.30
CHEMBL2037224 IC50 = 520.0 nM 6.28
CHEMBL2037194 IC50 = 600.0 nM 6.22
CHEMBL2037218 IC50 = 600.0 nM 6.22
CHEMBL2037213 IC50 = 610.0 nM 6.21
CHEMBL2037212 IC50 = 700.0 nM 6.16
CHEMBL2037193 IC50 = 1000.0 nM 6.00
CHEMBL2037222 IC50 = 1300.0 nM 5.89
CHEMBL2037220 IC50 = 1500.0 nM 5.82
CHEMBL2037217 IC50 = 2200.0 nM 5.66
CHEMBL2037210 IC50 = 2800.0 nM 5.55
CHEMBL2037226 IC50 = 3000.0 nM 5.52
CHEMBL2037225 IC50 = 3300.0 nM 5.48
CHEMBL2037214 IC50 = 4900.0 nM 5.31
CHEMBL2037216 IC50 > 10000.0 nM -
CHEMBL2037219 IC50 > 10000.0 nM -