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Compound Detail

CHEMBL152514

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CC(=N)N1CCC(Oc2ccc3c(c2)OCC(=O)N3Cc2cccc(-c3cccc(C(=N)N)c3)c2)CC1

Basic Information

ChEMBL ID CHEMBL152514
Phase Preclinical
Structure Type MOL
InChI Key PHDWMIRCMOIKBY-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

497.6
MW (Da)
4.40
ALogP
5
HBA
3
HBD
115.7
PSA (Ų)
0.34
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 C29H31N5O3
MW 497.60
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -0.69

Activity Summary

IC50 2 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 8.4 8.4 4.0 1
Trypsin II
CHEMBL4290
IC50 6.84 6.84 143.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 4.0 nM 8.4 Inhibitory concentration to factor Xa 12565972
Trypsin II IC50 = 143.0 nM 6.84 Inhibitory concentration against trypsin 12565972

Literature References

PubMed DOI Target Context # Activities
12565972 10.1016/s0960-894x(02)00927-7 Coagulation factor X 1
12565972 10.1016/s0960-894x(02)00927-7 Prothrombin 1
12565972 10.1016/s0960-894x(02)00927-7 Trypsin II 1
12565972 10.1016/s0960-894x(02)00927-7 Unchecked 1

Data from ChEMBL 36 via Core Engine