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Assay Detail

CHEMBL4186501

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

Binding
Inhibition of TNAP (unknown origin) using PPi as substrate
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alkaline phosphatase, tissue-nonspecific isozyme (CHEMBL5979)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 5-((5-chloro-2-methoxyphenyl)sulfonamido)nicotinamide (SBI-425), a potent and orally bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor.
Pinkerton AB, Sergienko E, Bravo Y, Dahl R, Ma CT, Sun Q, Jackson MR, Cosford NDP, Millán JL.
Bioorg Med Chem Lett (2018) 28 : 31 -34
PubMed 29174347 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 6.89 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1569928 1 8.22
CHEMBL569639 1 8.22
CHEMBL4214913 1 7.85
CHEMBL567850 1 7.82
CHEMBL4208605 1 7.80
CHEMBL4217036 1 7.72
CHEMBL4213116 1 7.64
CHEMBL4215759 1 7.58
CHEMBL4216295 1 7.42
CHEMBL1569953 1 7.37
CHEMBL4206067 1 7.19
CHEMBL4216888 1 7.14
CHEMBL4217814 1 7.14
CHEMBL4214312 1 7.14
CHEMBL4210692 1 7.08
CHEMBL4205359 1 6.96
CHEMBL4217588 1 6.92
CHEMBL4210124 1 6.88
CHEMBL4202840 1 6.87
CHEMBL4215202 1 6.83
CHEMBL4217835 1 6.80
CHEMBL4217772 1 6.75
CHEMBL4213236 1 6.74
CHEMBL4213086 1 6.71
CHEMBL4209321 1 6.70
CHEMBL4216913 1 6.51
CHEMBL4204021 1 6.49
CHEMBL4217934 1 6.37
CHEMBL4204197 1 6.17
CHEMBL4205652 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1569928 IC50 = 6.0 nM 8.22
CHEMBL569639 IC50 = 6.0 nM 8.22
CHEMBL4214913 IC50 = 14.0 nM 7.85
CHEMBL567850 IC50 = 15.0 nM 7.82
CHEMBL4208605 IC50 = 16.0 nM 7.80
CHEMBL4217036 IC50 = 19.0 nM 7.72
CHEMBL4213116 IC50 = 23.0 nM 7.64
CHEMBL4215759 IC50 = 26.0 nM 7.58
CHEMBL4216295 IC50 = 38.0 nM 7.42
CHEMBL1569953 IC50 = 43.0 nM 7.37
CHEMBL4206067 IC50 = 65.0 nM 7.19
CHEMBL4216888 IC50 = 73.0 nM 7.14
CHEMBL4217814 IC50 = 73.0 nM 7.14
CHEMBL4214312 IC50 = 73.0 nM 7.14
CHEMBL4210692 IC50 = 84.0 nM 7.08
CHEMBL4205359 IC50 = 109.0 nM 6.96
CHEMBL4217588 IC50 = 120.0 nM 6.92
CHEMBL4210124 IC50 = 131.0 nM 6.88
CHEMBL4202840 IC50 = 134.0 nM 6.87
CHEMBL4215202 IC50 = 147.0 nM 6.83
CHEMBL4217835 IC50 = 160.0 nM 6.80
CHEMBL4217772 IC50 = 178.0 nM 6.75
CHEMBL4213236 IC50 = 183.0 nM 6.74
CHEMBL4213086 IC50 = 193.0 nM 6.71
CHEMBL4209321 IC50 = 198.0 nM 6.70
CHEMBL4216913 IC50 = 310.0 nM 6.51
CHEMBL4204021 IC50 = 322.0 nM 6.49
CHEMBL4217934 IC50 = 432.0 nM 6.37
CHEMBL4204197 IC50 = 671.0 nM 6.17
CHEMBL4205652 IC50 = 876.0 nM 6.06
CHEMBL4212628 IC50 = 896.0 nM 6.05
CHEMBL4212086 IC50 = 1490.0 nM 5.83
CHEMBL4206103 IC50 = 1510.0 nM 5.82
CHEMBL4209407 IC50 = 4170.0 nM 5.38
CHEMBL1566142 IC50 = 10300.0 nM 4.99