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Assay Detail

CHEMBL2066761

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Binding
Inhibition of swine H+/K+-ATPase after 30 mins by colorimetry
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of a novel pyrrole derivative 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine fumarate (TAK-438) as a potassium-competitive acid blocker (P-CAB).
Arikawa Y, Nishida H, Kurasawa O, Hasuoka A, Hirase K, Inatomi N, Hori Y, Matsukawa J, Imanishi A, Kondo M, Tarui N, Hamada T, Takagi T, Takeuchi T, Kajino M.
J Med Chem (2012) 55 : 4446 -4456
PubMed 22512618 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.33 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2064023 1 7.96
CHEMBL2064031 1 7.89
CHEMBL2064027 1 7.80
CHEMBL3217004 1 7.80
CHEMBL3217002 1 7.77
CHEMBL2064032 VONOPRAZAN FUMARATE 4.0 1 7.72
CHEMBL2064033 1 7.70
CHEMBL2064022 1 7.52
CHEMBL3217005 1 7.47
CHEMBL3215887 1 7.34
CHEMBL2064036 1 7.34
CHEMBL2064025 1 7.29
CHEMBL3217003 1 7.12
CHEMBL2064024 1 7.11
CHEMBL2064026 1 6.96
CHEMBL2064028 1 6.77
CHEMBL2064038 1 6.64
CHEMBL2064165 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2064023 IC50 = 11.0 nM 7.96
CHEMBL2064031 IC50 = 13.0 nM 7.89
CHEMBL2064027 IC50 = 16.0 nM 7.80
CHEMBL3217004 IC50 = 16.0 nM 7.80
CHEMBL3217002 IC50 = 17.0 nM 7.77
CHEMBL2064032 VONOPRAZAN FUMARATE IC50 = 19.0 nM 7.72
CHEMBL2064033 IC50 = 20.0 nM 7.70
CHEMBL2064022 IC50 = 30.0 nM 7.52
CHEMBL3217005 IC50 = 34.0 nM 7.47
CHEMBL3215887 IC50 = 46.0 nM 7.34
CHEMBL2064036 IC50 = 46.0 nM 7.34
CHEMBL2064025 IC50 = 51.0 nM 7.29
CHEMBL3217003 IC50 = 75.0 nM 7.12
CHEMBL2064024 IC50 = 78.0 nM 7.11
CHEMBL2064026 IC50 = 110.0 nM 6.96
CHEMBL2064028 IC50 = 170.0 nM 6.77
CHEMBL2064038 IC50 = 230.0 nM 6.64
CHEMBL2064165 IC50 = 2200.0 nM 5.66