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Assay Detail

CHEMBL4002822

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

ADMET
Inhibition of platelet NHE1 in human platelet rich plasma assessed as decrease in platelet swelling preincubated for 3 mins followed by sodium propionate addition measured after 4 mins by spectrophotometric method
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium/hydrogen exchanger 1 (CHEMBL2781)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Sodium hydrogen exchanger inhibitory activity of benzotriazole derivatives.
Singh D, Silakari O.
Eur J Med Chem (2017) 126 : 183 -189
PubMed 27750152 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 4.36 6.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL436559 CARIPORIDE 2.0 1 6.76
CHEMBL4071353 1 4.30
CHEMBL4095965 1 4.29
CHEMBL1288725 1 4.29
CHEMBL4082866 1 4.23
CHEMBL4072374 1 4.22
CHEMBL557236 1 4.20
CHEMBL4074684 1 4.19
CHEMBL945 AMILORIDE 4.0 1 4.18
CHEMBL425230 1 4.17
CHEMBL4084954 1 4.16
CHEMBL1884989 1 4.14
CHEMBL204234 1 4.14
CHEMBL4097403 1 4.06
CHEMBL3086212 1 4.01
CHEMBL4085368 1 -
CHEMBL4093129 1 -
CHEMBL4072288 1 -
CHEMBL4087253 1 -
CHEMBL4079373 1 -
CHEMBL4068558 1 -
CHEMBL84963 BENZOTRIAZOLE 1 -
CHEMBL4100842 1 -
CHEMBL4063302 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL436559 CARIPORIDE IC50 = 172.0 nM 6.76
CHEMBL4071353 IC50 = 49950.0 nM 4.30
CHEMBL4095965 IC50 = 50890.0 nM 4.29
CHEMBL1288725 IC50 = 51570.0 nM 4.29
CHEMBL4082866 IC50 = 59230.0 nM 4.23
CHEMBL4072374 IC50 = 60590.0 nM 4.22
CHEMBL557236 IC50 = 63470.0 nM 4.20
CHEMBL4074684 IC50 = 65140.0 nM 4.19
CHEMBL945 AMILORIDE IC50 = 66730.0 nM 4.18
CHEMBL425230 IC50 = 68110.0 nM 4.17
CHEMBL4084954 IC50 = 69750.0 nM 4.16
CHEMBL1884989 IC50 = 72510.0 nM 4.14
CHEMBL204234 IC50 = 72380.0 nM 4.14
CHEMBL4097403 IC50 = 86480.0 nM 4.06
CHEMBL3086212 IC50 = 97100.0 nM 4.01
CHEMBL4085368 IC50 = 191230.0 nM -
CHEMBL4093129 IC50 = 154670.0 nM -
CHEMBL4072288 IC50 = 101120.0 nM -
CHEMBL4087253 IC50 = 135000.0 nM -
CHEMBL4079373 IC50 = 355000.0 nM -
CHEMBL4068558 IC50 = 177000.0 nM -
CHEMBL84963 BENZOTRIAZOLE IC50 = 192680.0 nM -
CHEMBL4100842 IC50 = 156540.0 nM -
CHEMBL4063302 IC50 = 115250.0 nM -