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Assay Detail

CHEMBL864198

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

Binding
Inhibition of human beta tryptase
35
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tryptase beta-1 (CHEMBL2617)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of novel, potent, and selective human beta-tryptase inhibitors based on alpha-keto-[1,2,4]-oxadiazoles.
Lee CS, Liu W, Sprengeler PA, Somoza JR, Janc JW, Sperandio D, Spencer JR, Green MJ, McGrath ME.
Bioorg Med Chem Lett (2006) 16 : 4036 -4040
PubMed 16714109 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 35 8.03 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL211357 1 8.82
CHEMBL212774 1 8.77
CHEMBL380293 1 8.77
CHEMBL213928 1 8.74
CHEMBL377890 1 8.74
CHEMBL377656 1 8.72
CHEMBL209395 1 8.72
CHEMBL214136 1 8.70
CHEMBL379528 1 8.68
CHEMBL213951 1 8.62
CHEMBL214368 1 8.55
CHEMBL214367 1 8.54
CHEMBL379561 1 8.52
CHEMBL213780 1 8.49
CHEMBL188069 1 8.46
CHEMBL276908 1 8.44
CHEMBL213927 2 8.43
CHEMBL378244 1 8.24
CHEMBL377619 1 8.09
CHEMBL210129 1 8.00
CHEMBL211638 1 7.96
CHEMBL209604 1 7.96
CHEMBL426330 1 7.92
CHEMBL213779 1 7.89
CHEMBL379486 1 7.80
CHEMBL213778 1 7.47
CHEMBL386704 1 7.43
CHEMBL211585 1 7.41
CHEMBL214148 1 7.22
CHEMBL214149 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL211357 Ki = 1.5 nM 8.82
CHEMBL380293 Ki = 1.7 nM 8.77
CHEMBL212774 Ki = 1.7 nM 8.77
CHEMBL213928 Ki = 1.8 nM 8.74
CHEMBL377890 Ki = 1.8 nM 8.74
CHEMBL377656 Ki = 1.9 nM 8.72
CHEMBL209395 Ki = 1.9 nM 8.72
CHEMBL214136 Ki = 2.0 nM 8.70
CHEMBL379528 Ki = 2.1 nM 8.68
CHEMBL213951 Ki = 2.4 nM 8.62
CHEMBL214368 Ki = 2.8 nM 8.55
CHEMBL214367 Ki = 2.9 nM 8.54
CHEMBL379561 Ki = 3.0 nM 8.52
CHEMBL213780 Ki = 3.2 nM 8.49
CHEMBL188069 Ki = 3.5 nM 8.46
CHEMBL276908 Ki = 3.6 nM 8.44
CHEMBL213927 Ki = 3.7 nM 8.43
CHEMBL213927 Ki = 3.7 nM 8.43
CHEMBL378244 Ki = 5.8 nM 8.24
CHEMBL377619 Ki = 8.2 nM 8.09
CHEMBL210129 Ki = 9.9 nM 8.00
CHEMBL209604 Ki = 11.0 nM 7.96
CHEMBL211638 Ki = 11.0 nM 7.96
CHEMBL426330 Ki = 12.0 nM 7.92
CHEMBL213779 Ki = 13.0 nM 7.89
CHEMBL379486 Ki = 16.0 nM 7.80
CHEMBL213778 Ki = 34.0 nM 7.47
CHEMBL386704 Ki = 37.0 nM 7.43
CHEMBL211585 Ki = 39.0 nM 7.41
CHEMBL214148 Ki = 60.0 nM 7.22
CHEMBL214149 Ki = 140.0 nM 6.85
CHEMBL414865 Ki = 220.0 nM 6.66
CHEMBL213554 Ki = 230.0 nM 6.64
CHEMBL378910 Ki = 470.0 nM 6.33
CHEMBL213698 Ki = 770.0 nM 6.11