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Compound Detail

CHEMBL562620

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COc1ccccc1N1CCN(Cc2cc3ccccn3n2)CC1

Basic Information

ChEMBL ID CHEMBL562620
Phase Preclinical
Structure Type MOL
InChI Key PONADOYAURXJAH-UHFFFAOYSA-N
4
Targets
21
Activities
1
Assay Types
0
PK Parameters
5
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 -1.71

Activity Summary

Ki 21 meas. best 8.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(4) dopamine receptor
CHEMBL219
Ki 8.92 8.78 1.2 2
D(3) dopamine receptor
CHEMBL234
Ki 7.36 6.4789 44.0 9
Unchecked
CHEMBL612545
Ki 7.34 6.7286 46.0 7
D(2) dopamine receptor
CHEMBL217
Ki 6.55 6.15 280.0 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
D(4) dopamine receptor Ki = 1.2 nM 8.92 Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed i... 19606869
D(4) dopamine receptor Ki = 2.3 nM 8.64 Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor e... 19606869
D(3) dopamine receptor Ki = 44.0 nM 7.36 Displacement of [3H]spiperone from human cloned dopamine D3 receptor FV3.28,3.29... 19606869
Unchecked Ki = 46.0 nM 7.34 Displacement of [3H]spiperone from human cloned dopamine D2L receptor FV3.28,3.2... 19606869
D(3) dopamine receptor Ki = 51.0 nM 7.29 Displacement of [3H]spiperone from human cloned dopamine D3 receptor V2.61F/FV3.... 19606869
Unchecked Ki = 54.0 nM 7.27 Displacement of [3H]spiperone from human cloned dopamine D2L receptor V2.61F/FV3... 19606869
D(3) dopamine receptor Ki = 61.0 nM 7.21 Displacement of [3H]spiperone from human cloned dopamine D3 receptor H6.55A muta... 19606869
Unchecked Ki = 63.0 nM 7.2 Displacement of [3H]spiperone from human cloned dopamine D2L receptor H6.55A mut... 19606869
Unchecked Ki = 94.0 nM 7.03 Displacement of [3H]spiperone from human cloned dopamine D2L receptor V2.61F mut... 19606869
D(2) dopamine receptor Ki = 280.0 nM 6.55 Displacement of [3H]spiperone from human cloned dopamine D2L receptor expressed ... 19606869
D(3) dopamine receptor Ki = 340.0 nM 6.47 Displacement of [3H]spiperone from human cloned dopamine D3 receptor V180E/S182I... 19606869
D(2) dopamine receptor Ki = 350.0 nM 6.46 Displacement of [3H]spiperone from wild type human cloned dopamine D2L receptor ... 19606869
Unchecked Ki = 590.0 nM 6.23 Displacement of [3H]spiperone from human cloned dopamine D2L receptor H6.55F mut... 19606869
Unchecked Ki = 610.0 nM 6.21 Displacement of [3H]spiperone from human cloned dopamine D2L receptor L2.64F mut... 19606869
D(3) dopamine receptor Ki = 680.0 nM 6.17 Displacement of [3H]spiperone from human cloned dopamine D3 receptor D3.32E muta... 19606869
D(3) dopamine receptor Ki = 720.0 nM 6.14 Displacement of [3H]spiperone from human cloned dopamine D3 receptor L2.64F muta... 19606869
D(3) dopamine receptor Ki = 770.0 nM 6.11 Displacement of [3H]spiperone from wild type human cloned dopamine D3 receptor e... 19606869
D(3) dopamine receptor Ki = 1200.0 nM 5.92 Displacement of [3H]spiperone from human cloned dopamine D3 receptor expressed i... 19606869
Unchecked Ki = 1500.0 nM 5.82 Displacement of [3H]spiperone from human cloned dopamine D2L receptor D3.32E mut... 19606869
D(3) dopamine receptor Ki = 2300.0 nM 5.64 Displacement of [3H]spiperone from human cloned dopamine D3 receptor V2.61F muta... 19606869

Literature References

PubMed DOI Target Context # Activities
19606869 10.1021/jm900690y Unchecked 24
19606869 10.1021/jm900690y D(3) dopamine receptor 9
19606869 10.1021/jm900690y D(2) dopamine receptor 3
19606869 10.1021/jm900690y D(4) dopamine receptor 2
19606869 10.1021/jm900690y Dopamine receptors; D3 & D4 1

Data from ChEMBL 36 via Core Engine