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Assay Detail

CHEMBL839521

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

Binding
Binding affinity value against kallikrein
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Kallikrein-1 (CHEMBL2319)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
Bruncko M, McClellan WJ, Wendt MD, Sauer DR, Geyer A, Dalton CR, Kaminski MA, Weitzberg M, Gong J, Dellaria JF, Mantei R, Zhao X, Nienaber VL, Stewart K, Klinghofer V, Bouska J, Rockway TW, Giranda VL.
Bioorg Med Chem Lett (2005) 15 : 93 -98
PubMed 15582418 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.43 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL362600 1 7.38
CHEMBL182959 1 7.27
CHEMBL360195 1 7.08
CHEMBL104505 1 7.00
CHEMBL181595 1 6.81
CHEMBL182303 1 6.69
CHEMBL319047 1 6.58
CHEMBL182547 1 6.53
CHEMBL182460 1 6.47
CHEMBL181599 1 6.42
CHEMBL179941 1 6.28
CHEMBL185515 1 6.24
CHEMBL183021 1 6.19
CHEMBL360703 1 6.11
CHEMBL182220 1 6.00
CHEMBL185345 1 6.00
CHEMBL182309 1 5.85
CHEMBL426433 1 5.61
CHEMBL104937 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL362600 Ki = 42.0 nM 7.38
CHEMBL182959 Ki = 54.0 nM 7.27
CHEMBL360195 Ki = 83.0 nM 7.08
CHEMBL104505 Ki = 100.0 nM 7.00
CHEMBL181595 Ki = 156.0 nM 6.81
CHEMBL182303 Ki = 206.0 nM 6.69
CHEMBL319047 Ki = 265.0 nM 6.58
CHEMBL182547 Ki = 295.0 nM 6.53
CHEMBL182460 Ki = 336.0 nM 6.47
CHEMBL181599 Ki = 379.0 nM 6.42
CHEMBL179941 Ki = 525.0 nM 6.28
CHEMBL185515 Ki = 576.0 nM 6.24
CHEMBL183021 Ki = 640.0 nM 6.19
CHEMBL360703 Ki = 770.0 nM 6.11
CHEMBL182220 Ki = 992.0 nM 6.00
CHEMBL185345 Ki = 991.0 nM 6.00
CHEMBL182309 Ki = 1402.0 nM 5.85
CHEMBL426433 Ki = 2482.0 nM 5.61
CHEMBL104937 Ki = 2500.0 nM 5.60