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Compound Detail

CHEMBL3277935

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Cl.N=C(N)c1ccc(OCc2cccc(-c3cccc(COc4ccc(C(=N)N)cc4Br)c3)c2)c(Br)c1

Basic Information

ChEMBL ID CHEMBL3277935
Phase Preclinical
Structure Type MOL
InChI Key JESMXUYIYCTMNQ-UHFFFAOYSA-N
Parent Compound CHEMBL3245422
Active Moiety CHEMBL3245422
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

608.3
MW (Da)
6.60
ALogP
4
HBA
4
HBD
118.2
PSA (Ų)
0.13
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H25Br2ClN4O2
MW 644.80
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -0.28

Activity Summary

Ki 3 meas. best 6.6
IC50 1 meas. best 5.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 6.6 6.6 250.0 1
Prothrombin
CHEMBL4471
Ki 6.57 6.57 270.0 1
Glandular kallikrein
CHEMBL3243909
Ki 5.66 5.66 2200.0 1
Prothrombin
CHEMBL204
IC50 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
1271404 10.1021/jm00227a011 Prothrombin 2
1271404 10.1021/jm00227a011 Glandular kallikrein 1
1271404 10.1021/jm00227a011 Unchecked 1
1271404 10.1021/jm00227a011 Plasma 1

Data from ChEMBL 36 via Core Engine