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Assay Detail

CHEMBL4407673

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

ADMET
Inhibition of His-tagged human TrkC expressed in baculovirus expression system using Tyr1 peptide as substrate after 1.5 hrs by FRET-based Z-LYTE assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

NT-3 growth factor receptor (CHEMBL5608)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-Amino-2,3-dihydro-1<i>H</i>-indene-5-carboxamide-Based Discoidin Domain Receptor 1 (DDR1) Inhibitors: Design, Synthesis, and in Vivo Antipancreatic Cancer Efficacy.
Zhu D, Huang H, Pinkas DM, Luo J, Ganguly D, Fox AE, Arner E, Xiang Q, Tu ZC, Bullock AN, Brekken RA, Ding K, Lu X.
J Med Chem (2019) 62 : 7431 -7444
PubMed 31310125 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.77 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4553037 1 7.52
CHEMBL4472914 1 7.33
CHEMBL4472004 1 6.80
CHEMBL4441609 1 6.67
CHEMBL4570381 1 6.56
CHEMBL4541139 1 6.44
CHEMBL4437631 1 6.10
CHEMBL4482862 1 -
CHEMBL4568103 1 -
CHEMBL4558430 1 -
CHEMBL4443543 1 -
CHEMBL4470262 1 -
CHEMBL4585974 1 -
CHEMBL4560079 1 -
CHEMBL4574620 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4553037 IC50 = 30.2 nM 7.52
CHEMBL4472914 IC50 = 46.3 nM 7.33
CHEMBL4472004 IC50 = 158.9 nM 6.80
CHEMBL4441609 IC50 = 215.4 nM 6.67
CHEMBL4570381 IC50 = 278.0 nM 6.56
CHEMBL4541139 IC50 = 364.2 nM 6.44
CHEMBL4437631 IC50 = 790.0 nM 6.10
CHEMBL4482862 IC50 > 1000.0 nM -
CHEMBL4568103 IC50 > 1000.0 nM -
CHEMBL4558430 IC50 > 1000.0 nM -
CHEMBL4443543 IC50 > 1000.0 nM -
CHEMBL4470262 IC50 > 1000.0 nM -
CHEMBL4585974 IC50 > 1000.0 nM -
CHEMBL4560079 IC50 > 1000.0 nM -
CHEMBL4574620 IC50 > 1000.0 nM -