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Compound Detail

CHEMBL1800526

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COc1ccnc(CCc2nc3cc(Br)cnc3[nH]2)c1

Basic Information

ChEMBL ID CHEMBL1800526
Phase Preclinical
Structure Type MOL
InChI Key NCNCDRDHFQNSFX-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
3
PK Parameters
5
Publications
0
Known Names

Molecular Properties

333.2
MW (Da)
2.91
ALogP
4
HBA
1
HBD
63.7
PSA (Ų)
0.80
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H13BrN4O
MW 333.19
Aromatic Rings 3
Heavy Atoms 20
NP-Likeness -1.28

Activity Summary

IC50 3 meas. best 6.73

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nitric oxide synthase, inducible
CHEMBL4481
IC50 6.73 6.73 186.2 1
Nitric oxide synthase 1
CHEMBL3568
IC50 5.08 5.08 8317.6 1
Nitric oxide synthase 3
CHEMBL4803
IC50 4.06 4.06 87096.4 1

Pharmacokinetic Data

Parameter Value Units Species
CL 3.2 uL.min-1.(10^6cells)-1 Homo sapiens
CL 23.5 mL.min-1.g-1 Homo sapiens
CL 29.0 uL.min-1.(10^6cells)-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3301361 ADMET 4
21684157 10.1016/j.bmcl.2011.05.073 Nitric oxide synthase, inducible 1
21684157 10.1016/j.bmcl.2011.05.073 Nitric oxide synthase 3 1
21684157 10.1016/j.bmcl.2011.05.073 Nitric oxide synthase 1 1
- 10.6019/CHEMBL3301361 No relevant target 1

Data from ChEMBL 36 via Core Engine