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Assay Detail

CHEMBL898074

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Binding
Inhibition of human factor 10a
ChEMBL ↗
75
Total Activities
74
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa.
Qiao JX, Chang CH, Cheney DL, Morin PE, Wang GZ, King SR, Wang TC, Rendina AR, Luettgen JM, Knabb RM, Wexler RR, Lam PY.
Bioorg Med Chem Lett (2007) 17 : 4419 -4427
PubMed 17588746 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 75 7.85 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL231779 APIXABAN 4.0 1 10.10
CHEMBL558198 RAZAXABAN HYDROCHLORIDE -1.0 1 9.72
CHEMBL233992 — — 1 9.37
CHEMBL400227 — — 1 9.36
CHEMBL450578 — — 1 9.29
CHEMBL398380 — — 1 9.17
CHEMBL401024 — — 1 9.15
CHEMBL233754 — — 1 9.03
CHEMBL234590 — — 1 9.02
CHEMBL233984 — — 2 9.00
CHEMBL233994 — — 1 9.00
CHEMBL233543 — — 1 8.96
CHEMBL393815 — — 1 8.89
CHEMBL231940 — — 1 8.89
CHEMBL399593 — — 1 8.82
CHEMBL232566 — — 1 8.82
CHEMBL393421 — — 1 8.77
CHEMBL233542 — — 1 8.74
CHEMBL231748 — — 1 8.68
CHEMBL398795 — — 1 8.64
CHEMBL427952 — — 1 8.62
CHEMBL393814 — — 1 8.60
CHEMBL233755 — — 1 8.59
CHEMBL427842 — — 1 8.59
CHEMBL398998 — — 1 8.55
CHEMBL234812 — — 1 8.49
CHEMBL231787 — — 1 8.43
CHEMBL231961 — — 1 8.41
CHEMBL233964 — — 1 8.40
CHEMBL400816 — — 1 8.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL231779 APIXABAN Ki = 0.08 nM 10.10
CHEMBL558198 RAZAXABAN HYDROCHLORIDE Ki = 0.19 nM 9.72
CHEMBL233992 — Ki = 0.43 nM 9.37
CHEMBL400227 — Ki = 0.44 nM 9.36
CHEMBL450578 — Ki = 0.51 nM 9.29
CHEMBL398380 — Ki = 0.67 nM 9.17
CHEMBL401024 — Ki = 0.71 nM 9.15
CHEMBL233754 — Ki = 0.94 nM 9.03
CHEMBL234590 — Ki = 0.95 nM 9.02
CHEMBL233984 — Ki = 1.0 nM 9.00
CHEMBL233994 — Ki = 1.0 nM 9.00
CHEMBL233543 — Ki = 1.1 nM 8.96
CHEMBL393815 — Ki = 1.3 nM 8.89
CHEMBL231940 — Ki = 1.3 nM 8.89
CHEMBL232566 — Ki = 1.5 nM 8.82
CHEMBL399593 — Ki = 1.5 nM 8.82
CHEMBL393421 — Ki = 1.7 nM 8.77
CHEMBL233542 — Ki = 1.8 nM 8.74
CHEMBL231748 — Ki = 2.1 nM 8.68
CHEMBL398795 — Ki = 2.3 nM 8.64
CHEMBL427952 — Ki = 2.4 nM 8.62
CHEMBL393814 — Ki = 2.5 nM 8.60
CHEMBL233755 — Ki = 2.6 nM 8.59
CHEMBL427842 — Ki = 2.6 nM 8.59
CHEMBL398998 — Ki = 2.8 nM 8.55
CHEMBL234812 — Ki = 3.2 nM 8.49
CHEMBL231787 — Ki = 3.7 nM 8.43
CHEMBL233984 — Ki = 3.8 nM 8.42
CHEMBL231961 — Ki = 3.9 nM 8.41
CHEMBL233964 — Ki = 4.0 nM 8.40
CHEMBL233173 — Ki = 4.2 nM 8.38
CHEMBL400816 — Ki = 4.2 nM 8.38
CHEMBL400226 — Ki = 4.4 nM 8.36
CHEMBL393521 — Ki = 4.7 nM 8.33
CHEMBL231751 — Ki = 4.8 nM 8.32
CHEMBL233963 — Ki = 5.0 nM 8.30
CHEMBL234172 — Ki = 7.1 nM 8.15
CHEMBL391527 — Ki = 7.3 nM 8.14
CHEMBL232325 — Ki = 7.92 nM 8.10
CHEMBL428899 — Ki = 8.1 nM 8.09
CHEMBL231750 — Ki = 10.0 nM 8.00
CHEMBL440969 — Ki = 10.0 nM 8.00
CHEMBL231726 — Ki = 13.0 nM 7.89
CHEMBL231749 — Ki = 13.0 nM 7.89
CHEMBL233131 — Ki = 14.0 nM 7.85
CHEMBL430164 — Ki = 16.0 nM 7.80
CHEMBL439054 — Ki = 17.0 nM 7.77
CHEMBL233332 — Ki = 20.0 nM 7.70
CHEMBL233806 — Ki = 23.0 nM 7.64
CHEMBL232323 — Ki = 27.0 nM 7.57