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Assay Detail

CHEMBL981501

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

Binding
Inhibition of human factor 10a
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa.
Nagata T, Yoshino T, Haginoya N, Yoshikawa K, Nagamochi M, Kobayashi S, Komoriya S, Yokomizo A, Muto R, Yamaguchi M, Osanai K, Suzuki M, Kanno H.
Bioorg Med Chem (2009) 17 : 1193 -1206
PubMed 19128974 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 8.34 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL516922 1 8.74
CHEMBL473243 1 8.66
CHEMBL508906 1 8.64
CHEMBL479863 1 8.64
CHEMBL474459 1 8.60
CHEMBL515569 1 8.59
CHEMBL515895 1 8.54
CHEMBL516195 1 8.47
CHEMBL480637 1 8.46
CHEMBL514798 1 8.46
CHEMBL479661 1 8.38
CHEMBL473856 1 8.35
CHEMBL479662 1 8.27
CHEMBL538657 1 8.12
CHEMBL479860 1 7.92
CHEMBL245678 1 7.80
CHEMBL19902 DX-9065A 1 7.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL516922 IC50 = 1.8 nM 8.74
CHEMBL473243 IC50 = 2.2 nM 8.66
CHEMBL508906 IC50 = 2.3 nM 8.64
CHEMBL479863 IC50 = 2.3 nM 8.64
CHEMBL474459 IC50 = 2.5 nM 8.60
CHEMBL515569 IC50 = 2.6 nM 8.59
CHEMBL515895 IC50 = 2.9 nM 8.54
CHEMBL516195 IC50 = 3.4 nM 8.47
CHEMBL480637 IC50 = 3.5 nM 8.46
CHEMBL514798 IC50 = 3.5 nM 8.46
CHEMBL479661 IC50 = 4.2 nM 8.38
CHEMBL473856 IC50 = 4.5 nM 8.35
CHEMBL479662 IC50 = 5.4 nM 8.27
CHEMBL538657 IC50 = 7.5 nM 8.12
CHEMBL479860 IC50 = 12.0 nM 7.92
CHEMBL245678 IC50 = 16.0 nM 7.80
CHEMBL19902 DX-9065A IC50 = 70.0 nM 7.16