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Assay Detail

CHEMBL986820

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

Binding
Activation of mouse wild type TRPV4 expressed in HEK293 cells assessed as increase in intracellular calcium concentration
11
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Modulation of the transient receptor potential vanilloid channel TRPV4 by 4alpha-phorbol esters: a structure-activity study.
Klausen TK, Pagani A, Minassi A, Ech-Chahad A, Prenen J, Owsianik G, Hoffmann EK, Pedersen SF, Appendino G, Nilius B.
J Med Chem (2009) 52 : 2933 -2939
PubMed 19361196 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 6.15 7.16
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL490470 2 7.16
CHEMBL504955 1 6.76
CHEMBL118987 1 6.43
CHEMBL541720 1 6.35
CHEMBL451849 1 5.55
CHEMBL27768 1 4.65
CHEMBL484343 1 -
CHEMBL507303 1 -
CHEMBL130626 1 -
CHEMBL504854 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL490470 EC50 = 70.0 nM 7.16
CHEMBL504955 EC50 = 175.0 nM 6.76
CHEMBL118987 EC50 = 370.0 nM 6.43
CHEMBL541720 EC50 = 450.0 nM 6.35
CHEMBL451849 EC50 = 2830.0 nM 5.55
CHEMBL27768 EC50 = 22470.0 nM 4.65
CHEMBL484343 EC50 > 50000.0 nM -
CHEMBL507303 EC50 > 50000.0 nM -
CHEMBL130626 EC50 > 50000.0 nM -
CHEMBL504854 EC50 > 50000.0 nM -
CHEMBL490470 Activity - -