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Assay Detail

CHEMBL4667323

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

Binding
Activation of human TREK2 by thallium flux mobilization assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Potassium channel subfamily K member 10 (CHEMBL2331041)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Towards a TREK-1/2 (TWIK-Related K+ Channel 1 and 2) dual activator tool compound: Multi-dimensional optimization of BL-1249.
Iwaki Y,Yashiro K,Kokubo M,Mori T,Wieting JM,McGowan KM,Bridges TM,Engers DW,Denton JS,Kurata H,Lindsley CW
Bioorg Med Chem Lett (2019) 29 : 1601 -1604
PubMed 31072652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 5.07 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4745050 1 5.30
CHEMBL4759521 1 5.26
CHEMBL4795261 1 5.25
CHEMBL4747631 1 5.23
CHEMBL4776102 1 5.17
CHEMBL4780579 1 5.12
CHEMBL1417584 1 5.11
CHEMBL4759642 1 5.11
CHEMBL4784090 1 4.58
CHEMBL4758530 1 4.54
CHEMBL4778307 1 -
CHEMBL4747514 1 -
CHEMBL4788471 1 -
CHEMBL4746675 1 -
CHEMBL4741520 1 -
CHEMBL4749533 1 -
CHEMBL4744719 1 -
CHEMBL4750436 1 -
CHEMBL4750599 1 -
CHEMBL4761929 1 -
CHEMBL4741659 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4745050 EC50 = 5000.0 nM 5.30
CHEMBL4759521 EC50 = 5500.0 nM 5.26
CHEMBL4795261 EC50 = 5600.0 nM 5.25
CHEMBL4747631 EC50 = 5900.0 nM 5.23
CHEMBL4776102 EC50 = 6800.0 nM 5.17
CHEMBL4780579 EC50 = 7500.0 nM 5.12
CHEMBL1417584 EC50 = 7700.0 nM 5.11
CHEMBL4759642 EC50 = 7700.0 nM 5.11
CHEMBL4784090 EC50 = 26500.0 nM 4.58
CHEMBL4758530 EC50 = 28500.0 nM 4.54
CHEMBL4778307 EC50 > 30000.0 nM -
CHEMBL4747514 EC50 > 30000.0 nM -
CHEMBL4788471 EC50 - -
CHEMBL4746675 EC50 - -
CHEMBL4741520 EC50 - -
CHEMBL4749533 EC50 - -
CHEMBL4744719 EC50 - -
CHEMBL4750436 EC50 > 30000.0 nM -
CHEMBL4750599 EC50 < 3600.0 nM -
CHEMBL4761929 EC50 - -
CHEMBL4741659 EC50 > 30000.0 nM -