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Compound Detail

CHEMBL561763

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CSc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1

Basic Information

ChEMBL ID CHEMBL561763
Phase Preclinical
Structure Type MOL
InChI Key ZMVDAQVAKLTNRL-UHFFFAOYSA-N
4
Targets
21
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

409.6
MW (Da)
3.00
ALogP
6
HBA
1
HBD
52.9
PSA (Ų)
0.48
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 C22H27N5OS
MW 409.56
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.89

Activity Summary

Ki 21 meas. best 10.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 10.0 7.5143 0.1 7
D(2) dopamine receptor
CHEMBL217
Ki 8.85 8.4033 1.4 3
D(3) dopamine receptor
CHEMBL234
Ki 8.47 7.2067 3.4 9
D(4) dopamine receptor
CHEMBL219
Ki 8.06 7.99 8.8 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked Ki = 0.1 nM 10.0 Displacement of [3H]spiperone from human cloned dopamine D2L receptor H6.55F mut... 19606869
D(2) dopamine receptor Ki = 1.4 nM 8.85 Displacement of [3H]spiperone from human cloned dopamine D2L receptor expressed ... 19606869
D(2) dopamine receptor Ki = 2.2 nM 8.66 Displacement of [3H]spiperone from wild type human cloned dopamine D2L receptor ... 19606869
D(3) dopamine receptor Ki = 3.4 nM 8.47 Displacement of [3H]spiperone from human cloned dopamine D3 receptor H6.55A muta... 19606869
D(3) dopamine receptor Ki = 8.0 nM 8.1 Displacement of [3H]spiperone from human cloned dopamine D3 receptor V180E/S182I... 19606869
D(4) dopamine receptor Ki = 8.8 nM 8.06 Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed i... 19606869
D(4) dopamine receptor Ki = 12.0 nM 7.92 Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor e... 19606869
D(3) dopamine receptor Ki = 17.0 nM 7.77 Displacement of [3H]spiperone from wild type human cloned dopamine D3 receptor e... 19606869
D(3) dopamine receptor Ki = 18.0 nM 7.75 Displacement of [3H]spiperone from human cloned dopamine D3 receptor expressed i... 19606869
D(2) dopamine receptor Ki = 20.0 nM 7.7 Displacement of [3H]spiperone from human cloned dopamine D2L receptor E181V/I183... 19606869
D(3) dopamine receptor Ki = 26.0 nM 7.58 Displacement of [3H]spiperone from human cloned dopamine D3 receptor D3.32E muta... 19606869
Unchecked Ki = 26.0 nM 7.58 Displacement of [3H]spiperone from human cloned dopamine D2L receptor D3.32E mut... 19606869
Unchecked Ki = 26.0 nM 7.58 Displacement of [3H]spiperone from human cloned dopamine D2L receptor H6.55A mut... 19606869
Unchecked Ki = 35.0 nM 7.46 Displacement of [3H]spiperone from human cloned dopamine D2L receptor V2.61F/FV3... 19606869
Unchecked Ki = 100.0 nM 7.0 Displacement of [3H]spiperone from human cloned dopamine D2L receptor L2.64F mut... 19606869
Unchecked Ki = 160.0 nM 6.8 Displacement of [3H]spiperone from human cloned dopamine D2L receptor V2.61F mut... 19606869
D(3) dopamine receptor Ki = 320.0 nM 6.5 Displacement of [3H]spiperone from human cloned dopamine D3 receptor V2.61F/FV3.... 19606869
D(3) dopamine receptor Ki = 430.0 nM 6.37 Displacement of [3H]spiperone from human cloned dopamine D3 receptor FV3.28,3.29... 19606869
D(3) dopamine receptor Ki = 650.0 nM 6.19 Displacement of [3H]spiperone from human cloned dopamine D3 receptor V2.61F muta... 19606869
Unchecked Ki = 660.0 nM 6.18 Displacement of [3H]spiperone from human cloned dopamine D2L receptor FV3.28,3.2... 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