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Assay Detail

CHEMBL4308449

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

Binding
Inhibition of human full length TRKA expressed in CHO cells assessed as decrease in NGF-induced Ca2+ flux by Calcium 4 dye-based FLIPR TETRA assay
113
Total Activities
113
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

Lead identification and characterization of hTrkA type 2 inhibitors.
Subramanian G, Zhu Y, Bowen SJ, Roush N, White JA, Huczek D, Zachary T, Javens C, Williams T, Janssen A, Gonzales A.
Bioorg Med Chem Lett (2019) 29 : 126680 -126680
PubMed 31610943 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 113 5.06 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4573890 1 7.05
CHEMBL4553953 1 6.65
CHEMBL4458913 1 6.58
CHEMBL4467890 1 6.40
CHEMBL4448181 1 6.27
CHEMBL4466950 1 6.18
CHEMBL4458775 1 6.17
CHEMBL4449741 1 6.14
CHEMBL4447061 1 6.08
CHEMBL4468419 1 6.07
CHEMBL4590914 1 6.01
CHEMBL4520451 1 5.84
CHEMBL4592814 1 5.80
CHEMBL4518353 1 5.71
CHEMBL4545062 1 5.63
CHEMBL4437226 1 5.60
CHEMBL4557960 1 5.60
CHEMBL4584518 1 5.56
CHEMBL4527557 1 5.52
CHEMBL4561854 1 5.50
CHEMBL4452210 1 5.46
CHEMBL4453384 1 5.41
CHEMBL4589260 1 5.37
CHEMBL4536149 1 5.35
CHEMBL4456764 1 5.30
CHEMBL4579460 1 5.28
CHEMBL4592731 1 5.27
CHEMBL4446374 1 5.25
CHEMBL4574513 1 5.24
CHEMBL4547987 1 5.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4573890 IC50 = 88.6 nM 7.05
CHEMBL4553953 IC50 = 221.6 nM 6.65
CHEMBL4458913 IC50 = 262.7 nM 6.58
CHEMBL4467890 IC50 = 401.5 nM 6.40
CHEMBL4448181 IC50 = 542.6 nM 6.27
CHEMBL4466950 IC50 = 658.2 nM 6.18
CHEMBL4458775 IC50 = 667.8 nM 6.17
CHEMBL4449741 IC50 = 718.2 nM 6.14
CHEMBL4447061 IC50 = 839.4 nM 6.08
CHEMBL4468419 IC50 = 849.0 nM 6.07
CHEMBL4590914 IC50 = 970.4 nM 6.01
CHEMBL4520451 IC50 = 1457.0 nM 5.84
CHEMBL4592814 IC50 = 1593.9 nM 5.80
CHEMBL4518353 IC50 = 1933.0 nM 5.71
CHEMBL4545062 IC50 = 2340.9 nM 5.63
CHEMBL4437226 IC50 = 2512.1 nM 5.60
CHEMBL4557960 IC50 = 2504.4 nM 5.60
CHEMBL4584518 IC50 = 2734.3 nM 5.56
CHEMBL4527557 IC50 = 2990.9 nM 5.52
CHEMBL4561854 IC50 = 3144.7 nM 5.50
CHEMBL4452210 IC50 = 3427.9 nM 5.46
CHEMBL4453384 IC50 = 3935.7 nM 5.41
CHEMBL4589260 IC50 = 4287.4 nM 5.37
CHEMBL4536149 IC50 = 4491.2 nM 5.35
CHEMBL4456764 IC50 = 5007.9 nM 5.30
CHEMBL4579460 IC50 = 5227.8 nM 5.28
CHEMBL4592731 IC50 = 5369.0 nM 5.27
CHEMBL4446374 IC50 = 5630.5 nM 5.25
CHEMBL4574513 IC50 = 5824.5 nM 5.24
CHEMBL4547987 IC50 = 6589.6 nM 5.18
CHEMBL4461469 IC50 = 6688.6 nM 5.17
CHEMBL4457208 IC50 = 7491.2 nM 5.12
CHEMBL4553513 IC50 = 7870.2 nM 5.10
CHEMBL4453991 IC50 = 8303.1 nM 5.08
CHEMBL4445789 IC50 = 10000.0 nM 5.00
CHEMBL4438018 IC50 = 10000.0 nM 5.00
CHEMBL4454504 IC50 = 10000.0 nM 5.00
CHEMBL4467067 IC50 = 10000.0 nM 5.00
CHEMBL4444056 IC50 = 10000.0 nM 5.00
CHEMBL4572771 IC50 = 10000.0 nM 5.00
CHEMBL4439853 IC50 = 10000.0 nM 5.00
CHEMBL4558108 IC50 = 10000.0 nM 5.00
CHEMBL4531238 IC50 = 10000.0 nM 5.00
CHEMBL4466570 IC50 = 10000.0 nM 5.00
CHEMBL4578725 IC50 = 10000.0 nM 5.00
CHEMBL4446114 IC50 = 10000.0 nM 5.00
CHEMBL4548111 IC50 = 10000.0 nM 5.00
CHEMBL4558719 IC50 = 10000.0 nM 5.00
CHEMBL4570112 IC50 = 10000.0 nM 5.00
CHEMBL4446168 IC50 = 10000.0 nM 5.00