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Compound Detail

CHEMBL513218

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C#Cc1ccc(NC(=O)c2cc(Cl)ccc2NC(=O)c2ccc(C(=N)N(C)C)cc2)nc1

Basic Information

ChEMBL ID CHEMBL513218
Phase Preclinical
Structure Type MOL
InChI Key VVQADOBQCCCLRJ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
4
Publications
0
Known Names

Molecular Properties

445.9
MW (Da)
4.11
ALogP
4
HBA
3
HBD
98.2
PSA (Ų)
0.31
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H20ClN5O2
MW 445.91
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.60

Activity Summary

IC50 1 meas. best 9.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 9.1 9.1 0.8 1

Pharmacokinetic Data

Parameter Value Units Species
CL 100.0 mL.min-1.kg-1 Rattus norvegicus
T1/2 2.0 hr Homo sapiens
T1/2 2.0 hr Rattus norvegicus
T1/2 6.3 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 0.8 nM 9.1 Inhibition of Factor 10a 19297154

Literature References

PubMed DOI Target Context # Activities
19297154 10.1016/j.bmcl.2009.02.111 ADMET 2
19297154 10.1016/j.bmcl.2009.02.111 Rattus norvegicus 2
19297154 10.1016/j.bmcl.2009.02.111 Coagulation factor X 1
19297154 10.1016/j.bmcl.2009.02.111 Plasma 1

Data from ChEMBL 36 via Core Engine