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Compound Detail

CHEMBL152599

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CC(=N)N1CCC(Oc2ccc3c(c2)OCC(=O)N3Cc2cc3ccc(C(=N)N)cc3n2C)CC1

Basic Information

ChEMBL ID CHEMBL152599
Phase Preclinical
Structure Type MOL
InChI Key DDWMFVRLSGMQCQ-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

474.6
MW (Da)
3.23
ALogP
6
HBA
3
HBD
120.7
PSA (Ų)
0.39
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 C26H30N6O3
MW 474.57
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.60

Activity Summary

IC50 3 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 8.7 8.7 2.0 1
Trypsin II
CHEMBL4290
IC50 7.12 7.12 76.0 1
Prothrombin
CHEMBL204
IC50 6.05 6.05 882.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 2.0 nM 8.7 Inhibitory concentration to factor Xa 12565972
Trypsin II IC50 = 76.0 nM 7.12 Inhibitory concentration against trypsin 12565972
Prothrombin IC50 = 882.0 nM 6.05 Inhibition of factor II 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