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Compound Detail

CHEMBL3966335

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CCOc1cc(OC2CCN(C)CC2)c(F)c([C@@H](Nc2ccc(C(=N)N)cc2)C(=O)O)c1

Basic Information

ChEMBL ID CHEMBL3966335
Phase Preclinical
Structure Type MOL
InChI Key UJHGDHHSUXVKDH-OAQYLSRUSA-N
2
Targets
14
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

444.5
MW (Da)
3.22
ALogP
6
HBA
4
HBD
120.9
PSA (Ų)
0.35
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H29FN4O4
MW 444.51
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -0.65

Activity Summary

IC50 12 meas. best 6.15
Kd 2 meas. best 6.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL5062
Kd 6.85 6.85 141.3 1
Coagulation factor X
CHEMBL244
Kd 6.55 6.55 284.0 1
Coagulation factor X
CHEMBL244
IC50 6.15 6.0033 706.0 12

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Kd = 141.33 nM 6.85 Protein construct Rabbit Factor Xa purchased from Enzyme Research Laboratories ... -
Coagulation factor X Kd = 284.0 nM 6.55 Protein construct Factor Xa purchased from R&D Systems- Source : Sf9 derived, M... -
Coagulation factor X IC50 = 706.0 nM 6.15 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 736.0 nM 6.13 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 764.0 nM 6.12 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 901.0 nM 6.04 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 992.0 nM 6.0 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 1010.0 nM 6.0 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 1030.0 nM 5.99 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 1030.0 nM 5.99 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 1060.0 nM 5.97 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 1090.0 nM 5.96 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 1360.0 nM 5.87 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 1500.0 nM 5.82 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3885741 Coagulation factor X 19

Data from ChEMBL 36 via Core Engine