Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL212631

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1

Basic Information

ChEMBL ID CHEMBL212631
Phase Preclinical
Structure Type MOL
InChI Key QGLGNPCWSBQHAU-UHFFFAOYSA-N
7
Targets
13
Activities
2
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

322.4
MW (Da)
2.67
ALogP
5
HBA
0
HBD
33.0
PSA (Ų)
0.74
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 C19H22N4O
MW 322.41
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -2.30

Activity Summary

Ki 11 meas. best 8.55
EC50 2 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(4) dopamine receptor
CHEMBL219
Ki 8.55 8.55 2.8 2
D(4) dopamine receptor
CHEMBL219
EC50 8.52 8.435 3.0 2
Adrenergic receptor alpha-1
CHEMBL2094251
Ki 7.01 7.01 98.0 1
D(2) dopamine receptor
CHEMBL217
Ki 6.96 6.3475 110.0 4
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 5.66 5.66 2200.0 1
D(3) dopamine receptor
CHEMBL234
Ki 5.41 5.41 3900.0 1
5-hydroxytryptamine receptor 2A
CHEMBL2490
Ki 5.23 5.23 5900.0 1
D(1A) dopamine receptor
CHEMBL5067
Ki 4.7 4.7 20000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
D(4) dopamine receptor Ki = 2.8 nM 8.55 Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell memb... 16789750
D(4) dopamine receptor Ki = 2.8 nM 8.55 Agonist activity at dopamine D4 receptor (unknown origin) 31404862
D(4) dopamine receptor EC50 = 3.0 nM 8.52 Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 1... 16789750
D(4) dopamine receptor EC50 = 4.5 nM 8.35 Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation... 16789750
Adrenergic receptor alpha-1 Ki = 98.0 nM 7.01 Displacement of [3H]prazosin from porcine Adrenergic alpha-1 receptor in porcine... 16789750
D(2) dopamine receptor Ki = 110.0 nM 6.96 Displacement of [3H]7-OH-DPAT from human dopamine receptor D2(long) in CHO cell ... 16789750
D(2) dopamine receptor Ki = 400.0 nM 6.4 Displacement of [3H]7-OH-DPAT from porcine dopamine receptor D2 16789750
D(2) dopamine receptor Ki = 930.0 nM 6.03 Displacement of [3H]spiperone from human dopamine receptor D2(short) in CHO cell... 16789750
D(2) dopamine receptor Ki = 990.0 nM 6.0 Displacement of [3H]spiperone from human dopamine receptor D2(long) in CHO cell ... 16789750
5-hydroxytryptamine receptor 1A Ki = 2200.0 nM 5.66 Displacement of [3H]8-OH-DPAT from 5HT1A receptor in porcine cortical membrane 16789750
D(3) dopamine receptor Ki = 3900.0 nM 5.41 Displacement of [3H]spiperone from human dopamine receptor D3 in CHO cell membra... 16789750
5-hydroxytryptamine receptor 2A Ki = 5900.0 nM 5.23 Displacement of [3H]ketanserin from 5HT2 receptor in porcine cortical membrane 16789750
D(1A) dopamine receptor Ki = 20000.0 nM 4.7 Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal memb... 16789750

Literature References

PubMed DOI Target Context # Activities
16789750 10.1021/jm060166w D(2) dopamine receptor 5
16789750 10.1021/jm060166w D(4) dopamine receptor 5
16789750 10.1021/jm060166w Rattus norvegicus 4
16789750 10.1021/jm060166w Dopamine receptors; D2 & D4 1
16789750 10.1021/jm060166w Adrenergic receptor alpha-1 1
16789750 10.1021/jm060166w 5-hydroxytryptamine receptor 2A 1
16789750 10.1021/jm060166w 5-hydroxytryptamine receptor 1A 1
16789750 10.1021/jm060166w D(3) dopamine receptor 1
16789750 10.1021/jm060166w D(1A) dopamine receptor 1
31404862 10.1016/j.ejmech.2019.111569 D(4) dopamine receptor 1

Data from ChEMBL 36 via Core Engine