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Compound Detail

CHEMBL301650

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O=c1[nH]cc(C(F)(F)F)c(=O)n1CCCN1CCN(c2ccccc2OCC(F)(F)F)CC1

Basic Information

ChEMBL ID CHEMBL301650
Phase Preclinical
Structure Type MOL
InChI Key CZJQYRRCGRRBAS-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

480.4
MW (Da)
2.71
ALogP
6
HBA
1
HBD
70.6
PSA (Ų)
0.62
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 C20H22F6N4O3
MW 480.41
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.43

Activity Summary

Ki 2 meas. best 8.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1B adrenergic receptor
CHEMBL232
Ki 8.2 8.2 6.3 1
Alpha-1A adrenergic receptor
CHEMBL229
Ki 7.7 7.7 19.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12749888 10.1016/s0960-894x(03)00305-6 Alpha-1A adrenergic receptor 2
12749888 10.1016/s0960-894x(03)00305-6 Alpha-1B adrenergic receptor 1
12749888 10.1016/s0960-894x(03)00305-6 Alpha-1D adrenergic receptor 1
12749888 10.1016/s0960-894x(03)00305-6 Adrenergic receptors; alpha-1 A & B 1

Data from ChEMBL 36 via Core Engine