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Assay Detail

CHEMBL815471

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

Binding
The inhibition constant against human trypsin
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Trypsin (CHEMBL2095204)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Tetrahydro-isoquinoline-based factor Xa inhibitors.
Kucznierz R, Grams F, Leinert H, Marzenell K, Engh RA, von der Saal W.
J Med Chem (1998) 41 : 4983 -4994
PubMed 9836616 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 5.66 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL147631 1 7.10
CHEMBL148357 1 6.70
CHEMBL144707 1 6.70
CHEMBL418849 1 6.70
CHEMBL146940 1 6.70
CHEMBL344281 1 6.40
CHEMBL147988 1 6.00
CHEMBL344309 1 5.70
CHEMBL539053 DX-9065A HYDROCHLORIDE HYDRATE 1 5.70
CHEMBL146097 1 5.70
CHEMBL344305 1 5.70
CHEMBL147436 1 5.52
CHEMBL357832 1 5.52
CHEMBL148972 1 5.30
CHEMBL144079 1 5.22
CHEMBL148323 1 5.22
CHEMBL144637 1 5.05
CHEMBL342568 1 5.00
CHEMBL358566 1 5.00
CHEMBL356973 1 5.00
CHEMBL439982 1 5.00
CHEMBL147789 1 5.00
CHEMBL148343 1 5.00
CHEMBL147707 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL147631 Ki = 80.0 nM 7.10
CHEMBL148357 Ki = 200.0 nM 6.70
CHEMBL144707 Ki = 200.0 nM 6.70
CHEMBL418849 Ki = 200.0 nM 6.70
CHEMBL146940 Ki = 200.0 nM 6.70
CHEMBL344281 Ki = 400.0 nM 6.40
CHEMBL147988 Ki = 1000.0 nM 6.00
CHEMBL344309 Ki = 2000.0 nM 5.70
CHEMBL539053 DX-9065A HYDROCHLORIDE HYDRATE Ki = 2000.0 nM 5.70
CHEMBL146097 Ki = 2000.0 nM 5.70
CHEMBL344305 Ki = 2000.0 nM 5.70
CHEMBL147436 Ki = 3000.0 nM 5.52
CHEMBL357832 Ki = 3000.0 nM 5.52
CHEMBL148972 Ki = 5000.0 nM 5.30
CHEMBL144079 Ki = 6000.0 nM 5.22
CHEMBL148323 Ki = 6000.0 nM 5.22
CHEMBL144637 Ki = 9000.0 nM 5.05
CHEMBL342568 Ki = 10000.0 nM 5.00
CHEMBL358566 Ki = 10000.0 nM 5.00
CHEMBL356973 Ki = 10000.0 nM 5.00
CHEMBL439982 Ki = 10000.0 nM 5.00
CHEMBL147789 Ki = 10000.0 nM 5.00
CHEMBL148343 Ki = 10000.0 nM 5.00
CHEMBL147707 Ki = 12000.0 nM 4.92