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Assay Detail

CHEMBL817288

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Binding
Inhibitory activity of compound against human tryptase was determined
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Tryptase (CHEMBL2095193)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase.
Bisacchi GS, Slusarchyk WA, Bolton SA, Hartl KS, Jacobs G, Mathur A, Meng W, Ogletree ML, Pi Z, Sutton JC, Treuner U, Zahler R, Zhao G, Seiler SM.
Bioorg Med Chem Lett (2004) 14 : 2227 -2231
PubMed 15081014 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.22 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70350 1 9.00
CHEMBL306448 1 8.74
CHEMBL302058 1 8.40
CHEMBL71037 1 8.40
CHEMBL441447 1 8.15
CHEMBL306696 1 7.72
CHEMBL72279 1 7.54
CHEMBL308109 1 7.52
CHEMBL70529 1 7.50
CHEMBL70666 1 7.47
CHEMBL70964 1 7.41
CHEMBL422412 1 7.21
CHEMBL305950 1 6.83
CHEMBL430999 1 6.68
CHEMBL307089 1 6.29
CHEMBL70619 1 5.98
CHEMBL273331 1 5.92
CHEMBL308015 1 5.58
CHEMBL70665 1 4.75
CHEMBL72282 1 -
CHEMBL303437 1 -
CHEMBL70738 1 -
CHEMBL303827 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70350 IC50 = 1.0 nM 9.00
CHEMBL306448 IC50 = 1.8 nM 8.74
CHEMBL302058 IC50 = 4.0 nM 8.40
CHEMBL71037 IC50 = 4.0 nM 8.40
CHEMBL441447 IC50 = 7.0 nM 8.15
CHEMBL306696 IC50 = 19.0 nM 7.72
CHEMBL72279 IC50 = 29.0 nM 7.54
CHEMBL308109 IC50 = 30.0 nM 7.52
CHEMBL70529 IC50 = 32.0 nM 7.50
CHEMBL70666 IC50 = 34.0 nM 7.47
CHEMBL70964 IC50 = 39.0 nM 7.41
CHEMBL422412 IC50 = 61.0 nM 7.21
CHEMBL305950 IC50 = 147.0 nM 6.83
CHEMBL430999 IC50 = 211.0 nM 6.68
CHEMBL307089 IC50 = 515.0 nM 6.29
CHEMBL70619 IC50 = 1053.0 nM 5.98
CHEMBL273331 IC50 = 1214.0 nM 5.92
CHEMBL308015 IC50 = 2605.0 nM 5.58
CHEMBL70665 IC50 = 17899.0 nM 4.75
CHEMBL72282 IC50 < 1.7 nM -
CHEMBL303437 IC50 < 1.7 nM -
CHEMBL70738 IC50 < 1.7 nM -
CHEMBL303827 IC50 > 33000.0 nM -