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Assay Detail

CHEMBL3887052

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

Binding
Inhibition Assay: Inhibition of human alpha-FXIIa was determined by the method described in [0092]-[0098] using activated human alpha-Factor XII (activated Hageman Factor) from Enzyme Research Laboratories at 50 mPEU/mL and CHA-Gly-Arg-pNA at 2 mM, 1 mM, and 0.5 mM as substrate; results are reported as Ki values (nanomolar).
17
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Coagulation factor XII (CHEMBL2821)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Trypsin-like serine protease inhibitors, and their preparation and use
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.02 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3660189 1 6.40
CHEMBL3660172 1 6.28
CHEMBL3660181 1 6.26
CHEMBL3660176 1 6.20
CHEMBL3660175 1 6.19
CHEMBL3660178 1 6.17
CHEMBL3660182 1 6.10
CHEMBL3660184 2 6.06
CHEMBL3660174 1 5.96
CHEMBL3660185 2 5.89
CHEMBL3660191 1 5.82
CHEMBL3660183 1 5.80
CHEMBL3660180 1 5.70
CHEMBL3660186 1 5.52
CHEMBL3660190 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3660189 Ki = 400.0 nM 6.40
CHEMBL3660172 Ki = 530.0 nM 6.28
CHEMBL3660181 Ki = 550.0 nM 6.26
CHEMBL3660176 Ki = 630.0 nM 6.20
CHEMBL3660175 Ki = 650.0 nM 6.19
CHEMBL3660178 Ki = 680.0 nM 6.17
CHEMBL3660182 Ki = 800.0 nM 6.10
CHEMBL3660184 Ki = 870.0 nM 6.06
CHEMBL3660184 Ki = 870.0 nM 6.06
CHEMBL3660174 Ki = 1100.0 nM 5.96
CHEMBL3660185 Ki = 1300.0 nM 5.89
CHEMBL3660185 Ki = 1300.0 nM 5.89
CHEMBL3660191 Ki = 1500.0 nM 5.82
CHEMBL3660183 Ki = 1600.0 nM 5.80
CHEMBL3660180 Ki = 2000.0 nM 5.70
CHEMBL3660186 Ki = 3000.0 nM 5.52
CHEMBL3660190 Ki > 10000.0 nM -