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Compound Detail

CHEMBL550453

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O=C(CN1C[C@H](NC(=O)c2ccc(Cl)s2)[C@@H](F)C1)Nc1ccc(-n2ccccc2=O)cc1F

Basic Information

ChEMBL ID CHEMBL550453
Phase Preclinical
Structure Type MOL
InChI Key SXIYSYYSKHUTQQ-RDJZCZTQSA-N
1
Targets
14
Activities
3
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

492.9
MW (Da)
3.08
ALogP
6
HBA
2
HBD
83.4
PSA (Ų)
0.55
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H19ClF2N4O3S
MW 492.94
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -2.19

Activity Summary

IC50 12 meas. best 8.23
Kd 1 meas. best 7.68
Ki 1 meas. best 7.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 8.23 8.1142 5.8 12
Coagulation factor X
CHEMBL244
Kd 7.68 7.68 21.0 1
Coagulation factor X
CHEMBL244
Ki 7.51 7.51 31.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 16.1 mL.min-1.g-1 Homo sapiens
CL 65.9 mL.min-1.g-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 5.82 nM 8.23 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 6.87 nM 8.16 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 7.15 nM 8.15 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 7.17 nM 8.14 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 7.53 nM 8.12 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 7.51 nM 8.12 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 7.82 nM 8.11 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 8.19 nM 8.09 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 8.11 nM 8.09 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 8.32 nM 8.08 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 8.65 nM 8.06 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X IC50 = 9.54 nM 8.02 Biochemical assay using fluorogenic peptide substrate.Step 1: Compound transfer ... -
Coagulation factor X Kd = 20.99 nM 7.68 Recombinant Factor Xa was immobilized on a Biacore CM5 chip at 25 degrees C with... -
Coagulation factor X Ki = 31.0 nM 7.51 Binding affinity to factor 10a 19200624

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3885741 Coagulation factor X 15
19200624 10.1016/j.ejmech.2008.12.025 Plasma 2
19200624 10.1016/j.ejmech.2008.12.025 ADMET 2
19200624 10.1016/j.ejmech.2008.12.025 Coagulation factor X 1

Data from ChEMBL 36 via Core Engine