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Assay Detail

CHEMBL4308450

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

Binding
Inhibition of human full length TRKB expressed in CHO cells assessed as decrease in NGF-induced Ca2+ flux by Calcium 4 dye-based FLIPR TETRA assay
ChEMBL ↗
114
Total Activities
114
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

BDNF/NT-3 growth factors receptor (CHEMBL4898) ↗
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 114 4.94 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4553953 — — 1 7.20
CHEMBL4573890 — — 1 6.45
CHEMBL4468419 — — 1 6.37
CHEMBL4458775 — — 1 6.11
CHEMBL4536149 — — 1 6.11
CHEMBL4461469 — — 1 5.92
CHEMBL4518353 — — 1 5.87
CHEMBL4545062 — — 1 5.69
CHEMBL4447061 — — 1 5.67
CHEMBL4437226 — — 1 5.60
CHEMBL4542472 — — 1 5.59
CHEMBL4518910 — — 1 5.55
CHEMBL4547987 — — 1 5.49
CHEMBL4446374 — — 1 5.45
CHEMBL4521004 — — 1 5.41
CHEMBL4584518 — — 1 5.34
CHEMBL4461532 — — 1 5.26
CHEMBL4448181 — — 1 5.17
CHEMBL4439176 — — 1 5.04
CHEMBL4458913 — — 1 5.03
CHEMBL4564272 — — 1 5.01
CHEMBL4578725 — — 1 5.00
CHEMBL4446114 — — 1 5.00
CHEMBL4558108 — — 1 5.00
CHEMBL4445789 — — 1 5.00
CHEMBL4531238 — — 1 5.00
CHEMBL4588390 — — 1 5.00
CHEMBL4532509 — — 1 5.00
CHEMBL4438018 — — 1 5.00
CHEMBL4558719 — — 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4553953 — IC50 = 63.7 nM 7.20
CHEMBL4573890 — IC50 = 358.6 nM 6.45
CHEMBL4468419 — IC50 = 423.2 nM 6.37
CHEMBL4458775 — IC50 = 771.0 nM 6.11
CHEMBL4536149 — IC50 = 778.0 nM 6.11
CHEMBL4461469 — IC50 = 1196.8 nM 5.92
CHEMBL4518353 — IC50 = 1340.8 nM 5.87
CHEMBL4545062 — IC50 = 2027.5 nM 5.69
CHEMBL4447061 — IC50 = 2138.5 nM 5.67
CHEMBL4437226 — IC50 = 2497.3 nM 5.60
CHEMBL4542472 — IC50 = 2594.4 nM 5.59
CHEMBL4518910 — IC50 = 2843.4 nM 5.55
CHEMBL4547987 — IC50 = 3224.9 nM 5.49
CHEMBL4446374 — IC50 = 3575.6 nM 5.45
CHEMBL4521004 — IC50 = 3886.6 nM 5.41
CHEMBL4584518 — IC50 = 4615.5 nM 5.34
CHEMBL4461532 — IC50 = 5460.3 nM 5.26
CHEMBL4448181 — IC50 = 6706.0 nM 5.17
CHEMBL4439176 — IC50 = 9064.5 nM 5.04
CHEMBL4458913 — IC50 = 9280.0 nM 5.03
CHEMBL4564272 — IC50 = 9792.4 nM 5.01
CHEMBL4454652 — IC50 = 10000.0 nM 5.00
CHEMBL4446114 — IC50 = 10000.0 nM 5.00
CHEMBL4558108 — IC50 = 10000.0 nM 5.00
CHEMBL4578725 — IC50 = 10000.0 nM 5.00
CHEMBL4454504 — IC50 = 10000.0 nM 5.00
CHEMBL4445789 — IC50 = 10000.0 nM 5.00
CHEMBL4531238 — IC50 = 10000.0 nM 5.00
CHEMBL4588390 — IC50 = 10000.0 nM 5.00
CHEMBL4467067 — IC50 = 10000.0 nM 5.00
CHEMBL4450466 — IC50 = 10000.0 nM 5.00
CHEMBL4570112 — IC50 = 10000.0 nM 5.00
CHEMBL4466570 — IC50 = 10000.0 nM 5.00
CHEMBL4532509 — IC50 = 10000.0 nM 5.00
CHEMBL4548111 — IC50 = 10000.0 nM 5.00
CHEMBL4446168 — IC50 = 10000.0 nM 5.00
CHEMBL4439853 — IC50 = 10000.0 nM 5.00
CHEMBL4572771 — IC50 = 10000.0 nM 5.00
CHEMBL4518108 — IC50 = 10000.0 nM 5.00
CHEMBL4444056 — IC50 = 10000.0 nM 5.00
CHEMBL4558719 — IC50 = 10000.0 nM 5.00
CHEMBL4472183 — IC50 = 10000.0 nM 5.00
CHEMBL4438018 — IC50 = 10000.0 nM 5.00
CHEMBL4443356 — IC50 = 20000.0 nM 4.70
CHEMBL4533532 — IC50 = 20000.0 nM 4.70
CHEMBL4463148 — IC50 = 20000.0 nM 4.70
CHEMBL4563845 — IC50 = 20000.0 nM 4.70
CHEMBL4444653 — IC50 = 20000.0 nM 4.70
CHEMBL4461600 — IC50 = 20000.0 nM 4.70
CHEMBL4545212 — IC50 = 20000.0 nM 4.70