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Assay Detail

CHEMBL5389737

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

Binding
Inhibition of FLAG-tagged mouse TRPM7 transfected in HEK293 cells assessed as inhibition of channel-mediated Mn2+ influx incubated for ~15 mins and measured for 90 secs by Fura-2-dye based fluorescence analysis
9
Total Activities
9
Compounds Tested
1
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

Transient Receptor Potential Melastatin 7 (TRPM7) Ion Channel Inhibitors: Preliminary SAR and Conformational Studies of Xenicane Diterpenoids from the Hawaiian Soft Coral <i>Sarcothelia edmondsoni</i>.
Yao G, Parris MR, Kuo WC, Pörzgen P, Castillo B, Mason ES, Chinchilla A, Huang J, Suzuki S, Ross R, Akana E, Vander Schuit S, Miller SP, Penner R, Sun HS, Feng ZP, Hull KG, Romo D, Fleig A, Horgen FD.
J Nat Prod (2024) 87 : 783 -797
PubMed 38537009 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.73 4.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5423236 1 4.92
CHEMBL5400468 1 4.89
CHEMBL5416180 1 4.70
CHEMBL5399993 1 4.70
CHEMBL169233 1 4.66
CHEMBL5420149 1 4.48
CHEMBL5426001 1 -
CHEMBL5408631 1 -
CHEMBL5436076 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5423236 IC50 = 12000.0 nM 4.92
CHEMBL5400468 IC50 = 13000.0 nM 4.89
CHEMBL5416180 IC50 = 20000.0 nM 4.70
CHEMBL5399993 IC50 = 20000.0 nM 4.70
CHEMBL169233 IC50 = 22000.0 nM 4.66
CHEMBL5420149 IC50 = 33000.0 nM 4.48
CHEMBL5426001 IC50 > 130000.0 nM -
CHEMBL5408631 IC50 > 150000.0 nM -
CHEMBL5436076 IC50 > 150000.0 nM -