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Compound Detail

CHEMBL550222

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CSc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1

Basic Information

ChEMBL ID CHEMBL550222
Phase Preclinical
Structure Type MOL
InChI Key DWEHMLBGRQZUJA-UHFFFAOYSA-N
4
Targets
21
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

423.6
MW (Da)
3.39
ALogP
6
HBA
1
HBD
52.9
PSA (Ų)
0.44
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H29N5OS
MW 423.59
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.86

Activity Summary

Ki 21 meas. best 9.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 9.46 7.91 0.3 9
D(4) dopamine receptor
CHEMBL219
Ki 9.2 8.195 0.6 2
Unchecked
CHEMBL612545
Ki 7.96 6.8929 11.0 7
D(2) dopamine receptor
CHEMBL217
Ki 7.8 7.6033 16.0 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
D(3) dopamine receptor Ki = 0.35 nM 9.46 Displacement of [3H]spiperone from human cloned dopamine D3 receptor expressed i... 19606869
D(3) dopamine receptor Ki = 0.5 nM 9.3 Displacement of [3H]spiperone from human cloned dopamine D3 receptor D3.32E muta... 19606869
D(4) dopamine receptor Ki = 0.63 nM 9.2 Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor e... 19606869
D(3) dopamine receptor Ki = 0.76 nM 9.12 Displacement of [3H]spiperone from human cloned dopamine D3 receptor H6.55A muta... 19606869
Unchecked Ki = 11.0 nM 7.96 Displacement of [3H]spiperone from human cloned dopamine D2L receptor H6.55F mut... 19606869
D(2) dopamine receptor Ki = 16.0 nM 7.8 Displacement of [3H]spiperone from human cloned dopamine D2L receptor expressed ... 19606869
D(3) dopamine receptor Ki = 18.0 nM 7.75 Displacement of [3H]spiperone from human cloned dopamine D3 receptor V2.61F/FV3.... 19606869
D(2) dopamine receptor Ki = 26.0 nM 7.58 Displacement of [3H]spiperone from human cloned dopamine D2L receptor E181V/I183... 19606869
D(3) dopamine receptor Ki = 33.0 nM 7.48 Displacement of [3H]spiperone from human cloned dopamine D3 receptor FV3.28,3.29... 19606869
D(2) dopamine receptor Ki = 37.0 nM 7.43 Displacement of [3H]spiperone from wild type human cloned dopamine D2L receptor ... 19606869
D(3) dopamine receptor Ki = 40.0 nM 7.4 Displacement of [3H]spiperone from human cloned dopamine D3 receptor V180E/S182I... 19606869
D(3) dopamine receptor Ki = 58.0 nM 7.24 Displacement of [3H]spiperone from human cloned dopamine D3 receptor L2.64F muta... 19606869
Unchecked Ki = 65.0 nM 7.19 Displacement of [3H]spiperone from human cloned dopamine D2L receptor V2.61F/FV3... 19606869
D(4) dopamine receptor Ki = 65.0 nM 7.19 Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed i... 19606869
Unchecked Ki = 120.0 nM 6.92 Displacement of [3H]spiperone from human cloned dopamine D2L receptor FV3.28,3.2... 19606869
Unchecked Ki = 130.0 nM 6.89 Displacement of [3H]spiperone from human cloned dopamine D2L receptor H6.55A mut... 19606869
Unchecked Ki = 130.0 nM 6.89 Displacement of [3H]spiperone from human cloned dopamine D2L receptor L2.64F mut... 19606869
D(3) dopamine receptor Ki = 160.0 nM 6.8 Displacement of [3H]spiperone from wild type human cloned dopamine D3 receptor e... 19606869
D(3) dopamine receptor Ki = 230.0 nM 6.64 Displacement of [3H]spiperone from human cloned dopamine D3 receptor V2.61F muta... 19606869
Unchecked Ki = 310.0 nM 6.51 Displacement of [3H]spiperone from human cloned dopamine D2L receptor D3.32E mut... 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