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Compound Detail

CHEMBL3217984

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CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3

Basic Information

ChEMBL ID CHEMBL3217984
Phase Preclinical
Structure Type MOL
InChI Key YVENIGOVHPMTDH-UHFFFAOYSA-N
24
Targets
24
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

308.4
MW (Da)
4.23
ALogP
3
HBA
0
HBD
6.5
PSA (Ų)
0.72
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H20N2S
MW 308.45
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -0.55

Activity Summary

Ki 24 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 8.7 8.7 2.0 1
Histamine H1 receptor
CHEMBL231
Ki 8.5 8.5 3.2 1
5-hydroxytryptamine receptor 2B
CHEMBL1833
Ki 8.3 8.3 5.0 1
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 8.1 8.1 7.9 1
5-hydroxytryptamine receptor 6
CHEMBL3371
Ki 7.8 7.8 15.8 1
D(1A) dopamine receptor
CHEMBL2056
Ki 7.6 7.6 25.1 1
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 7.5 7.5 31.6 1
D(3) dopamine receptor
CHEMBL234
Ki 7.5 7.5 31.6 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 7.4 7.4 39.8 1
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 7.2 7.2 63.1 1
5-hydroxytryptamine receptor 1D
CHEMBL1983
Ki 7.2 7.2 63.1 1
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 7.1 7.1 79.4 1
Histamine H2 receptor
CHEMBL1941
Ki 7.1 7.1 79.4 1
D(2) dopamine receptor
CHEMBL217
Ki 6.9 6.9 125.9 1
5-hydroxytryptamine receptor 5A
CHEMBL3426
Ki 6.7 6.7 199.5 1
D(4) dopamine receptor
CHEMBL219
Ki 6.7 6.7 199.5 1
Alpha-2B adrenergic receptor
CHEMBL1942
Ki 6.7 6.7 199.5 1
D(1B) dopamine receptor
CHEMBL1850
Ki 6.7 6.7 199.5 1
5-hydroxytryptamine receptor 1B
CHEMBL1898
Ki 6.5 6.5 316.2 1
Alpha-1A adrenergic receptor
CHEMBL229
Ki 6.3 6.3 501.2 1
5-hydroxytryptamine receptor 3A
CHEMBL1899
Ki 6.2 6.2 631.0 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 6.1 6.1 794.3 1
Muscarinic acetylcholine receptor M5
CHEMBL2035
Ki 6.1 6.1 794.3 1
5-hydroxytryptamine receptor 1E
CHEMBL2182
Ki 5.6 5.6 2511.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
5-hydroxytryptamine receptor 2A Ki = 1.995 nM 8.7 Binding affinity to serotonin 5-HT2A receptor (unknown origin) by PDSP assay -
Histamine H1 receptor Ki = 3.162 nM 8.5 Binding affinity to H1 histamine receptor (unknown origin) by PDSP assay -
5-hydroxytryptamine receptor 2B Ki = 5.012 nM 8.3 Binding affinity to serotonin 5-HT2B receptor (unknown origin) by PDSP assay -
5-hydroxytryptamine receptor 2C Ki = 7.943 nM 8.1 Binding affinity to serotonin 5-HT2C receptor (unknown origin) by PDSP assay -
5-hydroxytryptamine receptor 6 Ki = 15.85 nM 7.8 Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay -
D(1A) dopamine receptor Ki = 25.12 nM 7.6 Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assay -
D(3) dopamine receptor Ki = 31.62 nM 7.5 Binding affinity to dopamine D3 receptor (unknown origin) by PDSP assay -
Alpha-2C adrenergic receptor Ki = 31.62 nM 7.5 Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay -
5-hydroxytryptamine receptor 1A Ki = 39.81 nM 7.4 Binding affinity to serotonin 5-HT1A receptor (unknown origin) by PDSP assay -
5-hydroxytryptamine receptor 1D Ki = 63.1 nM 7.2 Binding affinity to serotonin 5-HT1D receptor (unknown origin) by PDSP assay -
Alpha-2A adrenergic receptor Ki = 63.1 nM 7.2 Binding affinity to adrenergic alpha2A receptor (unknown origin) by PDSP assay -
Histamine H2 receptor Ki = 79.43 nM 7.1 Binding affinity to H2 histamine receptor (unknown origin) by PDSP assay -
5-hydroxytryptamine receptor 7 Ki = 79.43 nM 7.1 Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay -
D(2) dopamine receptor Ki = 125.89 nM 6.9 Binding affinity to dopamine D2 receptor (unknown origin) by PDSP assay -
5-hydroxytryptamine receptor 5A Ki = 199.53 nM 6.7 Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay -
D(4) dopamine receptor Ki = 199.53 nM 6.7 Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assay -
D(1B) dopamine receptor Ki = 199.53 nM 6.7 Binding affinity to dopamine D5 receptor (unknown origin) by PDSP assay -
Alpha-2B adrenergic receptor Ki = 199.53 nM 6.7 Binding affinity to adrenergic alpha2B receptor (unknown origin) by PDSP assay -
5-hydroxytryptamine receptor 1B Ki = 316.23 nM 6.5 Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay -
Alpha-1A adrenergic receptor Ki = 501.19 nM 6.3 Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay -

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C2MD00311B Rattus norvegicus 5
- 10.1039/C2MD00311B 5-hydroxytryptamine receptor 2A 3
- 10.1039/C2MD00311B D(2) dopamine receptor 3
- 10.1039/C2MD00311B 5-hydroxytryptamine receptor 6 1
- 10.1039/C2MD00311B Alpha-1D adrenergic receptor 1
- 10.1039/C2MD00311B Alpha-1B adrenergic receptor 1
- 10.1039/C2MD00311B Alpha-1A adrenergic receptor 1
- 10.1039/C2MD00311B D(1B) dopamine receptor 1
- 10.1039/C2MD00311B D(4) dopamine receptor 1
- 10.1039/C2MD00311B D(3) dopamine receptor 1
- 10.1039/C2MD00311B D(1A) dopamine receptor 1
- 10.1039/C2MD00311B 5-hydroxytryptamine receptor 7 1
- 10.1039/C2MD00311B 5-hydroxytryptamine receptor 1A 1
- 10.1039/C2MD00311B 5-hydroxytryptamine receptor 5A 1
- 10.1039/C2MD00311B 5-hydroxytryptamine receptor 4 1
- 10.1039/C2MD00311B 5-hydroxytryptamine receptor 3A 1
- 10.1039/C2MD00311B 5-hydroxytryptamine receptor 2C 1
- 10.1039/C2MD00311B 5-hydroxytryptamine receptor 2B 1
- 10.1039/C2MD00311B 5-hydroxytryptamine receptor 1E 1
- 10.1039/C2MD00311B 5-hydroxytryptamine receptor 1D 1

Data from ChEMBL 36 via Core Engine