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Assay Detail

CHEMBL956028

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Binding
Inhibition of human Factor-10a
18
Total Activities
18
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

Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action.
Van Huis CA, Casimiro-Garcia A, Bigge CF, Cody WL, Dudley DA, Filipski KJ, Heemstra RJ, Kohrt JT, Leadley RJ, Narasimhan LS, McClanahan T, Mochalkin I, Pamment M, Peterson JT, Sahasrabudhe V, Schaum RP, Edmunds JJ.
Bioorg Med Chem (2009) 17 : 2501 -2511
PubMed 19231206 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 9.64 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL475682 1 10.70
CHEMBL476618 1 10.30
CHEMBL515107 1 10.10
CHEMBL474271 1 10.10
CHEMBL474678 1 10.00
CHEMBL514510 1 9.96
CHEMBL474070 1 9.80
CHEMBL475280 1 9.74
CHEMBL476412 1 9.74
CHEMBL515941 1 9.66
CHEMBL477229 1 9.51
CHEMBL448927 1 9.47
CHEMBL515156 1 9.30
CHEMBL515147 1 9.30
CHEMBL477228 1 9.27
CHEMBL476186 ERIBAXABAN 2.0 1 9.24
CHEMBL475481 1 8.92
CHEMBL476187 1 8.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL475682 IC50 = 0.02 nM 10.70
CHEMBL476618 IC50 = 0.05 nM 10.30
CHEMBL515107 IC50 = 0.08 nM 10.10
CHEMBL474271 IC50 = 0.08 nM 10.10
CHEMBL474678 IC50 = 0.1 nM 10.00
CHEMBL514510 IC50 = 0.11 nM 9.96
CHEMBL474070 IC50 = 0.16 nM 9.80
CHEMBL475280 IC50 = 0.18 nM 9.74
CHEMBL476412 IC50 = 0.18 nM 9.74
CHEMBL515941 IC50 = 0.22 nM 9.66
CHEMBL477229 IC50 = 0.31 nM 9.51
CHEMBL448927 IC50 = 0.34 nM 9.47
CHEMBL515156 IC50 = 0.5 nM 9.30
CHEMBL515147 IC50 = 0.5 nM 9.30
CHEMBL477228 IC50 = 0.54 nM 9.27
CHEMBL476186 ERIBAXABAN IC50 = 0.57 nM 9.24
CHEMBL475481 IC50 = 1.2 nM 8.92
CHEMBL476187 IC50 = 4.6 nM 8.34