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Assay Detail

CHEMBL657716

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

Binding
Binding affinity against human coagulation factor X
33
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Coagulation factor X (CHEMBL244)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of potent and selective amidino bicyclic factor Xa inhibitors.
Han Q, Dominguez C, Stouten PF, Park JM, Duffy DE, Galemmo RA, Rossi KA, Alexander RS, Smallwood AM, Wong PC, Wright MM, Luettgen JM, Knabb RM, Wexler RR.
J Med Chem (2000) 43 : 4398 -4415
PubMed 11087565 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 7.78 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL336661 2 9.49
CHEMBL138709 2 9.36
CHEMBL341920 1 9.22
CHEMBL136986 2 9.15
CHEMBL341979 2 9.15
CHEMBL136846 1 8.68
CHEMBL137499 1 8.64
CHEMBL343495 1 8.62
CHEMBL136215 2 8.51
CHEMBL136100 1 8.51
CHEMBL138956 1 8.47
CHEMBL342168 1 8.39
CHEMBL139063 1 8.20
CHEMBL139432 1 8.15
CHEMBL343380 1 8.10
CHEMBL138478 1 7.39
CHEMBL342036 1 7.05
CHEMBL139124 1 7.03
CHEMBL343784 1 6.92
CHEMBL140016 1 6.85
CHEMBL343827 1 6.66
CHEMBL139970 1 6.62
CHEMBL335340 1 6.40
CHEMBL337785 1 6.16
CHEMBL139682 1 5.66
CHEMBL136297 1 5.57
CHEMBL141259 1 5.41
CHEMBL136591 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL336661 Ki = 0.32 nM 9.49
CHEMBL336661 Ki = 0.32 nM 9.49
CHEMBL138709 Ki = 0.44 nM 9.36
CHEMBL341920 Ki = 0.6 nM 9.22
CHEMBL341979 Ki = 0.71 nM 9.15
CHEMBL136986 Ki = 0.7 nM 9.15
CHEMBL136986 Ki = 0.7 nM 9.15
CHEMBL138709 Ki = 0.92 nM 9.04
CHEMBL136846 Ki = 2.1 nM 8.68
CHEMBL137499 Ki = 2.3 nM 8.64
CHEMBL343495 Ki = 2.4 nM 8.62
CHEMBL136215 Ki = 3.1 nM 8.51
CHEMBL136215 Ki = 3.1 nM 8.51
CHEMBL136100 Ki = 3.1 nM 8.51
CHEMBL138956 Ki = 3.4 nM 8.47
CHEMBL342168 Ki = 4.1 nM 8.39
CHEMBL139063 Ki = 6.3 nM 8.20
CHEMBL139432 Ki = 7.0 nM 8.15
CHEMBL343380 Ki = 8.0 nM 8.10
CHEMBL138478 Ki = 41.0 nM 7.39
CHEMBL341979 Ki = 52.0 nM 7.28
CHEMBL342036 Ki = 89.0 nM 7.05
CHEMBL139124 Ki = 94.0 nM 7.03
CHEMBL343784 Ki = 120.0 nM 6.92
CHEMBL140016 Ki = 140.0 nM 6.85
CHEMBL343827 Ki = 220.0 nM 6.66
CHEMBL139970 Ki = 240.0 nM 6.62
CHEMBL335340 Ki = 400.0 nM 6.40
CHEMBL337785 Ki = 700.0 nM 6.16
CHEMBL139682 Ki = 2200.0 nM 5.66
CHEMBL136297 Ki = 2700.0 nM 5.57
CHEMBL141259 Ki = 3900.0 nM 5.41
CHEMBL136591 Ki = 11900.0 nM 4.92