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Compound Detail

CHEMBL144534

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COCC1=NC(C)=C(C(=O)OC)C(c2ccc(F)c(F)c2)N1CCCCCN1CCC(C#N)(c2ccccc2)CC1

Basic Information

ChEMBL ID CHEMBL144534
Phase Preclinical
Structure Type MOL
InChI Key LPTPYTCKPRTUIS-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

564.7
MW (Da)
5.54
ALogP
7
HBA
0
HBD
78.2
PSA (Ų)
0.26
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H38F2N4O3
MW 564.68
Aromatic Rings 2
Heavy Atoms 41
NP-Likeness -1.15

Activity Summary

Ki 3 meas. best 9.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
Ki 9.4 9.4 0.4 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 6.51 6.51 310.0 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 6.32 6.32 480.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10579843 10.1021/jm9902032 Alpha-1A adrenergic receptor 1
10579843 10.1021/jm9902032 Alpha-1B adrenergic receptor 1
10579843 10.1021/jm9902032 Alpha-1D adrenergic receptor 1
10579843 10.1021/jm9902032 Unchecked 1

Data from ChEMBL 36 via Core Engine