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Compound Detail

CHEMBL200153

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Cc1[nH]cnc1/C=C/CNC(=O)[C@@H]1CCCN1C(=O)[C@H](N)C(c1ccccc1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL200153
Phase Preclinical
Structure Type MOL
InChI Key MBNKUMIZUGCXRO-RJZIKQFVSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

457.6
MW (Da)
3.00
ALogP
4
HBA
3
HBD
104.1
PSA (Ų)
0.48
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H31N5O2
MW 457.58
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.28

Activity Summary

Ki 2 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 9.0 9.0 1.0 1
Trypsin
CHEMBL2095204
Ki 7.0 7.0 100.0 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 550.0 nM Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 1.0 nM 9.0 Binding affinity to thrombin 16257203
Trypsin Ki = 100.0 nM 7.0 Binding affinity to trypsin 16257203

Literature References

PubMed DOI Target Context # Activities
16257203 10.1016/j.bmcl.2005.09.083 Prothrombin 2
16257203 10.1016/j.bmcl.2005.09.083 Trypsin 1
16257203 10.1016/j.bmcl.2005.09.083 Canis familiaris 1

Data from ChEMBL 36 via Core Engine