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Assay Detail

CHEMBL847455

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Binding
In vitro inhibitory activity against thrombin(FIIa)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent and selective bicyclic lactam inhibitors of thrombin: Part 2: P1 modifications.
Plummer JS, Berryman KA, Cai C, Cody WL, DiMaio J, Doherty AM, Edmunds JJ, He JX, Holland DR, Levesque S, Kent DR, Narasimhan LS, Rubin JR, Rapundalo ST, Siddiqui MA, Susser AJ, St-Denis Y, Winocour PD.
Bioorg Med Chem Lett (1998) 8 : 3409 -3414
PubMed 9873743 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.58 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333154 1 9.00
CHEMBL324413 1 8.30
CHEMBL332716 1 7.52
CHEMBL3349354 1 7.48
CHEMBL115294 1 7.11
CHEMBL116297 1 6.86
CHEMBL115236 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333154 IC50 = 1.0 nM 9.00
CHEMBL324413 IC50 = 5.0 nM 8.30
CHEMBL332716 IC50 = 30.0 nM 7.52
CHEMBL3349354 IC50 = 33.0 nM 7.48
CHEMBL115294 IC50 = 77.0 nM 7.11
CHEMBL116297 IC50 = 137.0 nM 6.86
CHEMBL115236 IC50 = 150.0 nM 6.82