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Assay Detail

CHEMBL819079

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Binding
Binding affinity against thrombin
25
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prothrombin (CHEMBL204)
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 25 7.40 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2448441 1 9.00
CHEMBL36744 1 8.52
CHEMBL3349045 4 8.15
CHEMBL290577 1 8.15
CHEMBL286606 3 8.15
CHEMBL285285 1 7.75
CHEMBL288689 1 7.72
CHEMBL291026 3 7.72
CHEMBL288407 1 7.70
CHEMBL431115 1 7.68
CHEMBL288175 1 7.60
CHEMBL430545 1 7.54
CHEMBL287918 1 7.38
CHEMBL291085 1 7.37
CHEMBL291261 1 7.09
CHEMBL418050 1 6.89
CHEMBL36670 1 6.00
CHEMBL288150 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2448441 Ki = 1.0 nM 9.00
CHEMBL36744 Ki = 3.0 nM 8.52
CHEMBL3349045 Ki = 7.0 nM 8.15
CHEMBL3349045 Ki = 7.0 nM 8.15
CHEMBL3349045 Ki = 7.0 nM 8.15
CHEMBL286606 Ki = 7.0 nM 8.15
CHEMBL290577 Ki = 7.0 nM 8.15
CHEMBL285285 Ki = 18.0 nM 7.75
CHEMBL291026 Ki = 19.0 nM 7.72
CHEMBL288689 Ki = 19.0 nM 7.72
CHEMBL288407 Ki = 20.0 nM 7.70
CHEMBL431115 Ki = 21.0 nM 7.68
CHEMBL288175 Ki = 25.0 nM 7.60
CHEMBL291026 Ki = 26.0 nM 7.58
CHEMBL430545 Ki = 29.0 nM 7.54
CHEMBL287918 Ki = 42.0 nM 7.38
CHEMBL291085 Ki = 43.0 nM 7.37
CHEMBL291261 Ki = 82.0 nM 7.09
CHEMBL291026 Ki = 100.0 nM 7.00
CHEMBL3349045 Ki = 120.0 nM 6.92
CHEMBL418050 Ki = 130.0 nM 6.89
CHEMBL286606 Ki = 130.0 nM 6.89
CHEMBL36670 Ki = 1000.0 nM 6.00
CHEMBL288150 Ki = 11000.0 nM 4.96
CHEMBL286606 Ki = 15000.0 nM 4.82