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Assay Detail

CHEMBL4399998

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

Binding
Inhibition of recombinant full length human TrkA transfected in CHO cells assessed as inhibition of NGF-stimulated calcium influx by FLIPR assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

High affinity nerve growth factor receptor (CHEMBL2815)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Type 2 inhibitor leads of human tropomyosin receptor kinase (hTrkA).
Subramanian G, Bowen SJ, Zhu Y, Roush N, Zachary T, Javens C, Williams T, Janssen A, Gonzales A.
Bioorg Med Chem Lett (2019) 29 : 126624 -126624
PubMed 31444087 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.18 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4555143 1 7.50
CHEMBL4447685 1 7.06
CHEMBL4475899 1 6.11
CHEMBL4525857 1 5.58
CHEMBL4574596 1 5.39
CHEMBL4472006 1 5.30
CHEMBL1710419 1 5.18
CHEMBL4535656 1 5.00
CHEMBL4579301 1 4.70
CHEMBL4573099 1 4.70
CHEMBL4471969 1 4.70
CHEMBL1707321 1 4.70
CHEMBL4440941 1 4.70
CHEMBL4473447 1 4.70
CHEMBL4453766 1 4.70
CHEMBL4444267 1 4.70
CHEMBL4454926 1 4.70
CHEMBL4534509 1 4.70
CHEMBL4476611 1 4.70
CHEMBL4469499 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4555143 IC50 = 31.6 nM 7.50
CHEMBL4447685 IC50 = 86.5 nM 7.06
CHEMBL4475899 IC50 = 773.5 nM 6.11
CHEMBL4525857 IC50 = 2637.4 nM 5.58
CHEMBL4574596 IC50 = 4071.2 nM 5.39
CHEMBL4472006 IC50 = 5043.0 nM 5.30
CHEMBL1710419 IC50 = 6616.8 nM 5.18
CHEMBL4535656 IC50 = 10050.9 nM 5.00
CHEMBL4579301 IC50 = 20000.0 nM 4.70
CHEMBL4573099 IC50 = 20000.0 nM 4.70
CHEMBL4471969 IC50 = 20000.0 nM 4.70
CHEMBL1707321 IC50 = 20000.0 nM 4.70
CHEMBL4440941 IC50 = 20000.0 nM 4.70
CHEMBL4473447 IC50 = 20000.0 nM 4.70
CHEMBL4453766 IC50 = 20000.0 nM 4.70
CHEMBL4444267 IC50 = 20000.0 nM 4.70
CHEMBL4454926 IC50 = 20000.0 nM 4.70
CHEMBL4534509 IC50 = 20000.0 nM 4.70
CHEMBL4476611 IC50 = 20000.0 nM 4.70
CHEMBL4469499 IC50 = 20000.0 nM 4.70