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Assay Detail

CHEMBL701582

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

Binding
Binding affinity against kallikrein
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin.
Deadman JJ, Elgendy S, Goodwin CA, Green D, Baban JA, Patel G, Skordalakes E, Chino N, Claeson G, Kakkar VV.
J Med Chem (1995) 38 : 1511 -1522
PubMed 7739010 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.41 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3349045 1 8.21
CHEMBL418050 1 8.02
CHEMBL290577 1 8.02
CHEMBL36744 1 7.47
CHEMBL291026 1 6.92
CHEMBL287918 1 6.80
CHEMBL288176 1 6.43
CHEMBL291261 1 -
CHEMBL2448441 1 -
CHEMBL285285 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3349045 Ki = 6.1 nM 8.21
CHEMBL418050 Ki = 9.5 nM 8.02
CHEMBL290577 Ki = 9.5 nM 8.02
CHEMBL36744 Ki = 34.0 nM 7.47
CHEMBL291026 Ki = 120.0 nM 6.92
CHEMBL287918 Ki = 160.0 nM 6.80
CHEMBL288176 Ki = 370.0 nM 6.43
CHEMBL291261 Ki > 63.0 nM -
CHEMBL2448441 Ki = 0.0049 nM -
CHEMBL285285 Ki > 4.3 nM -