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Assay Detail

CHEMBL774080

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

Functional
Inhibition of 5-N-(ethyl isopropyl)-amiloride[EIPA]-sensitive Na+ uptake into acidified rabbit erythrocytes.
113
Total Activities
113
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Sodium/hydrogen exchanger (CHEMBL2096985)
Type PROTEIN FAMILY
Organism Oryctolagus cuniculus

Publication

(2-Methyl-5-(methylsulfonyl)benzoyl)guanidine Na+/H+ antiporter inhibitors.
Baumgarth M, Beier N, Gericke R.
J Med Chem (1997) 40 : 2017 -2034
PubMed 9207943 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 113 7.34 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64889 1 8.70
CHEMBL416314 1 8.32
CHEMBL292311 1 8.24
CHEMBL60551 1 8.23
CHEMBL59697 1 8.22
CHEMBL292105 1 8.17
CHEMBL64360 ENIPORIDE 2.0 1 8.10
CHEMBL303354 1 8.10
CHEMBL302450 1 8.09
CHEMBL302222 1 8.08
CHEMBL60249 1 8.06
CHEMBL62461 1 8.04
CHEMBL61271 1 8.03
CHEMBL294310 1 8.01
CHEMBL64359 1 8.00
CHEMBL64611 1 7.96
CHEMBL291658 1 7.96
CHEMBL64873 1 7.92
CHEMBL62385 1 7.92
CHEMBL304627 1 7.89
CHEMBL305087 1 7.89
CHEMBL418505 1 7.85
CHEMBL64747 1 7.85
CHEMBL294316 1 7.85
CHEMBL302914 1 7.85
CHEMBL64132 1 7.80
CHEMBL291353 1 7.80
CHEMBL293188 1 7.80
CHEMBL64469 1 7.72
CHEMBL59928 1 7.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64889 IC50 = 2.0 nM 8.70
CHEMBL416314 IC50 = 4.8 nM 8.32
CHEMBL292311 IC50 = 5.7 nM 8.24
CHEMBL60551 IC50 = 5.9 nM 8.23
CHEMBL59697 IC50 = 6.0 nM 8.22
CHEMBL292105 IC50 = 6.8 nM 8.17
CHEMBL303354 IC50 = 8.0 nM 8.10
CHEMBL64360 ENIPORIDE IC50 = 8.0 nM 8.10
CHEMBL302450 IC50 = 8.2 nM 8.09
CHEMBL302222 IC50 = 8.3 nM 8.08
CHEMBL60249 IC50 = 8.8 nM 8.06
CHEMBL62461 IC50 = 9.2 nM 8.04
CHEMBL61271 IC50 = 9.4 nM 8.03
CHEMBL294310 IC50 = 9.8 nM 8.01
CHEMBL64359 IC50 = 10.0 nM 8.00
CHEMBL64611 IC50 = 11.0 nM 7.96
CHEMBL291658 IC50 = 11.0 nM 7.96
CHEMBL62385 IC50 = 12.0 nM 7.92
CHEMBL64873 IC50 = 12.0 nM 7.92
CHEMBL305087 IC50 = 13.0 nM 7.89
CHEMBL304627 IC50 = 13.0 nM 7.89
CHEMBL418505 IC50 = 14.0 nM 7.85
CHEMBL64747 IC50 = 14.0 nM 7.85
CHEMBL302914 IC50 = 14.0 nM 7.85
CHEMBL294316 IC50 = 14.0 nM 7.85
CHEMBL293188 IC50 = 16.0 nM 7.80
CHEMBL291353 IC50 = 16.0 nM 7.80
CHEMBL64132 IC50 = 16.0 nM 7.80
CHEMBL64469 IC50 = 19.0 nM 7.72
CHEMBL59928 IC50 = 19.0 nM 7.72
CHEMBL446148 IC50 = 19.0 nM 7.72
CHEMBL61983 IC50 = 19.0 nM 7.72
CHEMBL61057 IC50 = 20.0 nM 7.70
CHEMBL60044 IC50 = 21.0 nM 7.68
CHEMBL423488 IC50 = 21.0 nM 7.68
CHEMBL62299 IC50 = 21.0 nM 7.68
CHEMBL64516 IC50 = 22.0 nM 7.66
CHEMBL62556 IC50 = 22.0 nM 7.66
CHEMBL62785 IC50 = 23.0 nM 7.64
CHEMBL65714 IC50 = 23.0 nM 7.64
CHEMBL59613 IC50 = 25.0 nM 7.60
CHEMBL64141 IC50 = 25.0 nM 7.60
CHEMBL60785 IC50 = 25.0 nM 7.60
CHEMBL62025 IC50 = 25.0 nM 7.60
CHEMBL436559 CARIPORIDE IC50 = 26.0 nM 7.58
CHEMBL64564 IC50 = 27.0 nM 7.57
CHEMBL65165 IC50 = 27.0 nM 7.57
CHEMBL294330 IC50 = 27.0 nM 7.57
CHEMBL302634 IC50 = 27.0 nM 7.57
CHEMBL424229 IC50 = 28.0 nM 7.55