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Compound Detail

CHEMBL3394388

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Cc1cc(N)nc(CCc2cc(CN)cc(CCc3ccc4cc[nH]c4n3)c2)c1

Basic Information

ChEMBL ID CHEMBL3394388
Phase Preclinical
Structure Type MOL
InChI Key WRRLIUHCTMZNNL-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

385.5
MW (Da)
3.88
ALogP
4
HBA
3
HBD
93.6
PSA (Ų)
0.45
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H27N5
MW 385.52
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -0.07

Activity Summary

Ki 3 meas. best 6.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nitric oxide synthase 1
CHEMBL3048
Ki 6.66 6.66 220.0 1
Nitric oxide synthase, inducible
CHEMBL3464
Ki 5.15 5.15 7098.0 1
Nitric oxide synthase 3
CHEMBL4802
Ki 4.28 4.28 52726.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Nitric oxide synthase 1 Ki = 220.0 nM 6.66 Inhibition of rat nNOS 25522110
Nitric oxide synthase, inducible Ki = 7098.0 nM 5.15 Inhibition of mouse iNOS 25522110
Nitric oxide synthase 3 Ki = 52726.0 nM 4.28 Inhibition of bovine eNOS 25522110

Literature References

PubMed DOI Target Context # Activities
25522110 10.1021/jm501723p Unchecked 5
25522110 10.1021/jm501723p Nitric oxide synthase, inducible 1
25522110 10.1021/jm501723p Nitric oxide synthase 3 1
25522110 10.1021/jm501723p Nitric oxide synthase 1 1

Data from ChEMBL 36 via Core Engine