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Compound Detail

CHEMBL268768

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COc1cc2nc(N3CCN(C(=O)/C=C/c4ccccc4)CC3)nc(N)c2cc1OC

Basic Information

ChEMBL ID CHEMBL268768
Phase Preclinical
Structure Type MOL
InChI Key IKWCRLCFRBNCER-CMDGGOBGSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

419.5
MW (Da)
2.59
ALogP
7
HBA
1
HBD
93.8
PSA (Ų)
0.64
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 C23H25N5O3
MW 419.49
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.70

Activity Summary

Kd 2 meas. best 9.38
IC50 1 meas. best 9.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL1907610
Kd 9.38 9.38 0.4 1
Adrenergic receptor alpha-1
CHEMBL1907610
IC50 9.16 9.16 0.7 1
Rattus norvegicus
CHEMBL376
Kd 9.14 9.14 0.7 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
6131135 10.1021/jm00357a016 Rattus norvegicus 26
2535878 10.1021/jm00121a020 Adrenergic receptor alpha-1 3
6131135 10.1021/jm00357a016 Unchecked 1

Data from ChEMBL 36 via Core Engine