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Assay Detail

CHEMBL1014656

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Binding
Inhibition of TNSALP
31
Total Activities
31
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Design and synthesis of pyrazole derivatives as potent and selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP).
Sidique S, Ardecky R, Su Y, Narisawa S, Brown B, Millán JL, Sergienko E, Cosford ND.
Bioorg Med Chem Lett (2009) 19 : 222 -225
PubMed 19038545 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 6.76 8.30
Ki 2 4.45 4.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL461194 1 8.30
CHEMBL450981 1 7.51
CHEMBL512931 1 7.46
CHEMBL466808 1 7.46
CHEMBL467008 1 7.36
CHEMBL467854 1 7.36
CHEMBL466809 1 7.34
CHEMBL459706 1 7.33
CHEMBL445965 1 7.29
CHEMBL511689 1 7.25
CHEMBL459707 1 7.09
CHEMBL501296 1 7.00
CHEMBL466992 1 6.92
CHEMBL459709 1 6.90
CHEMBL461425 1 6.87
CHEMBL459708 1 6.54
CHEMBL502169 1 6.49
CHEMBL445266 1 6.43
CHEMBL509575 1 6.40
CHEMBL507236 1 6.34
CHEMBL468685 1 6.31
CHEMBL467705 1 6.30
CHEMBL468052 1 6.30
CHEMBL468676 1 6.24
CHEMBL455023 1 6.08
CHEMBL505807 1 6.01
CHEMBL467382 1 5.89
CHEMBL468686 1 5.84
CHEMBL467853 1 5.31
CHEMBL1454 LEVAMISOLE 4.0 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL461194 IC50 = 5.0 nM 8.30
CHEMBL450981 IC50 = 31.0 nM 7.51
CHEMBL512931 IC50 = 35.0 nM 7.46
CHEMBL466808 IC50 = 35.0 nM 7.46
CHEMBL467008 IC50 = 44.0 nM 7.36
CHEMBL467854 IC50 = 44.0 nM 7.36
CHEMBL466809 IC50 = 46.0 nM 7.34
CHEMBL459706 IC50 = 47.0 nM 7.33
CHEMBL445965 IC50 = 51.0 nM 7.29
CHEMBL511689 IC50 = 56.0 nM 7.25
CHEMBL459707 IC50 = 82.0 nM 7.09
CHEMBL501296 IC50 = 100.0 nM 7.00
CHEMBL466992 IC50 = 119.0 nM 6.92
CHEMBL459709 IC50 = 127.0 nM 6.90
CHEMBL461425 IC50 = 134.0 nM 6.87
CHEMBL459708 IC50 = 285.0 nM 6.54
CHEMBL502169 IC50 = 324.0 nM 6.49
CHEMBL445266 IC50 = 375.0 nM 6.43
CHEMBL509575 IC50 = 398.0 nM 6.40
CHEMBL507236 IC50 = 459.0 nM 6.34
CHEMBL468685 IC50 = 488.0 nM 6.31
CHEMBL467705 IC50 = 500.0 nM 6.30
CHEMBL468052 IC50 = 500.0 nM 6.30
CHEMBL468676 IC50 = 574.0 nM 6.24
CHEMBL455023 IC50 = 828.0 nM 6.08
CHEMBL505807 IC50 = 980.0 nM 6.01
CHEMBL467382 IC50 = 1300.0 nM 5.89
CHEMBL468686 IC50 = 1450.0 nM 5.84
CHEMBL467853 IC50 = 4850.0 nM 5.31
CHEMBL1454 LEVAMISOLE Ki = 16000.0 nM 4.80
CHEMBL1355736 THEOPHYLLINE Ki = 82000.0 nM 4.09