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Assay Detail

CHEMBL860418

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

Binding
Binding affinity to trypsin
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Trypsin (CHEMBL2095204)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 1: Weakly basic azoles.
Isaacs RC, Solinsky MG, Cutrona KJ, Newton CL, Naylor-Olsen AM, Krueger JA, Lewis SD, Lucas BJ.
Bioorg Med Chem Lett (2006) 16 : 338 -342
PubMed 16257203 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 5.19 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200153 1 7.00
CHEMBL200573 1 6.85
CHEMBL371769 1 6.62
CHEMBL381205 1 5.64
CHEMBL96502 1 5.22
CHEMBL371650 1 5.19
CHEMBL200134 1 5.14
CHEMBL370557 1 5.02
CHEMBL200857 1 4.77
CHEMBL200593 1 4.68
CHEMBL199696 1 4.50
CHEMBL265363 1 4.44
CHEMBL373260 1 4.37
CHEMBL200674 1 4.23
CHEMBL199675 1 4.23
CHEMBL199609 1 -
CHEMBL200110 1 -
CHEMBL200920 1 -
CHEMBL200520 1 -
CHEMBL200504 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200153 Ki = 100.0 nM 7.00
CHEMBL200573 Ki = 140.0 nM 6.85
CHEMBL371769 Ki = 240.0 nM 6.62
CHEMBL381205 Ki = 2300.0 nM 5.64
CHEMBL96502 Ki = 6000.0 nM 5.22
CHEMBL371650 Ki = 6500.0 nM 5.19
CHEMBL200134 Ki = 7200.0 nM 5.14
CHEMBL370557 Ki = 9600.0 nM 5.02
CHEMBL200857 Ki = 17000.0 nM 4.77
CHEMBL200593 Ki = 21000.0 nM 4.68
CHEMBL199696 Ki = 32000.0 nM 4.50
CHEMBL265363 Ki = 36000.0 nM 4.44
CHEMBL373260 Ki = 43000.0 nM 4.37
CHEMBL200674 Ki = 59000.0 nM 4.23
CHEMBL199675 Ki = 59000.0 nM 4.23
CHEMBL199609 Ki = 178000.0 nM -
CHEMBL200110 Ki = 314000.0 nM -
CHEMBL200920 Ki > 1000000.0 nM -
CHEMBL200520 Ki = 124000.0 nM -
CHEMBL200504 Ki > 1000000.0 nM -