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Compound Detail

CHEMBL276013

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CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cc(C(C)(C)C)cc4[nH]cc(c34)C[C@H]2N(C)C1

Basic Information

ChEMBL ID CHEMBL276013
Phase Preclinical
Structure Type MOL
InChI Key BNMXUFDTDMYUGI-ZILOHOTNSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

481.7
MW (Da)
3.94
ALogP
4
HBA
2
HBD
71.7
PSA (Ų)
0.66
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H43N5O2
MW 481.69
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness 0.09

Activity Summary

IC50 5 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-2
CHEMBL2093864
IC50 8.15 8.15 7.0 1
5-hydroxytryptamine receptor 1A
CHEMBL273
IC50 7.05 7.05 90.0 1
Serotonin 2 (5-HT2) receptor
CHEMBL2093870
IC50 6.27 6.27 540.0 1
D(2) dopamine receptor
CHEMBL339
IC50 5.97 5.97 1060.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
IC50 5.53 5.53 2950.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9871719 10.1016/s0960-894x(98)00166-8 Adrenergic receptor alpha-1 1
9871719 10.1016/s0960-894x(98)00166-8 Adrenergic receptor alpha-2 1
9871719 10.1016/s0960-894x(98)00166-8 D(1A) dopamine receptor 1
9871719 10.1016/s0960-894x(98)00166-8 D(2) dopamine receptor 1
9871719 10.1016/s0960-894x(98)00166-8 5-hydroxytryptamine receptor 1A 1
9871719 10.1016/s0960-894x(98)00166-8 Serotonin 2 (5-HT2) receptor 1

Data from ChEMBL 36 via Core Engine