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Compound Detail

CHEMBL131495

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O=C1c2ccccc2C(=O)N1CCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1

Basic Information

ChEMBL ID CHEMBL131495
Phase Preclinical
Structure Type MOL
InChI Key NECJNLXOJRDELU-UHFFFAOYSA-N

Known Names

SLV-310
14
Targets
15
Activities
1
Assay Types
0
PK Parameters
17
Publications
1
Known Names

Molecular Properties

417.5
MW (Da)
4.47
ALogP
3
HBA
1
HBD
56.4
PSA (Ų)
0.48
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24FN3O2
MW 417.48
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.97

Activity Summary

Ki 15 meas. best 9.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent serotonin transporter
CHEMBL313
Ki 9.22 9.22 0.6 1
Sodium-dependent serotonin transporter
CHEMBL228
Ki 9.1 9.1 0.8 1
D(3) dopamine receptor
CHEMBL234
Ki 9.1 9.1 0.8 1
5-hydroxytryptamine receptor 2B
CHEMBL1833
Ki 8.8 8.8 1.6 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 8.6 8.6 2.5 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 8.5 8.5 3.2 1
D(2) dopamine receptor
CHEMBL217
Ki 8.5 8.15 3.2 2
Histamine H1 receptor
CHEMBL3943
Ki 7.5 7.5 31.6 1
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 7.4 7.4 39.8 1
D(4) dopamine receptor
CHEMBL219
Ki 7.1 7.1 79.4 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 7.0 7.0 100.0 1
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 7.0 7.0 100.0 1
Adrenergic receptor alpha-2
CHEMBL2093864
Ki 6.6 6.6 251.2 1
5-hydroxytryptamine receptor 6
CHEMBL3371
Ki 6.4 6.4 398.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sodium-dependent serotonin transporter Ki = 0.6 nM 9.22 In vitro binding affinity for serotonin reuptake sites in rat frontal cortex mem... 12565939
D(3) dopamine receptor Ki = 0.7943 nM 9.1 Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO c... 17880057
Sodium-dependent serotonin transporter Ki = 0.7943 nM 9.1 Displacement of [3H]paraxetine from human 5HT transporter expressed in HEK293 ce... 17880057
5-hydroxytryptamine receptor 2B Ki = 1.585 nM 8.8 Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cells 17880057
5-hydroxytryptamine receptor 1A Ki = 2.512 nM 8.6 Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells 17880057
D(2) dopamine receptor Ki = 3.162 nM 8.5 Displacement of [3H]spiperone from human dopamine D2 receptor short form express... 17880057
Adrenergic receptor alpha-1 Ki = 3.162 nM 8.5 Displacement of [3H]prazosin from adrenergic alpha1 receptor in rat cerebral cor... 17880057
D(2) dopamine receptor Ki = 16.0 nM 7.8 In vitro binding affinity at human cloned dopamine receptor D2 (long) stably exp... 12565939
Histamine H1 receptor Ki = 31.62 nM 7.5 Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebel... 17880057
5-hydroxytryptamine receptor 2C Ki = 39.81 nM 7.4 Displacement of [3H]mesulergine from 5HT2C receptor expressed in CHO cells 17880057
D(4) dopamine receptor Ki = 79.43 nM 7.1 Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO... 17880057
5-hydroxytryptamine receptor 2A Ki = 100.0 nM 7.0 Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells 17880057
5-hydroxytryptamine receptor 7 Ki = 100.0 nM 7.0 Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells 17880057
Adrenergic receptor alpha-2 Ki = 251.19 nM 6.6 Displacement of [3H]RX 821002 from adrenergic alpha-2 receptor in rat cerebral c... 17880057
5-hydroxytryptamine receptor 6 Ki = 398.11 nM 6.4 Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells 17880057

Literature References

PubMed DOI Target Context # Activities
17880057 10.1021/jm070516u 5-hydroxytryptamine receptor 2C 1
17880057 10.1021/jm070516u Histamine H1 receptor 1
17880057 10.1021/jm070516u Adrenergic receptor alpha-2 1
17880057 10.1021/jm070516u Adrenergic receptor alpha-1 1
17880057 10.1021/jm070516u Muscarinic acetylcholine receptor M4 1
17880057 10.1021/jm070516u Muscarinic acetylcholine receptor M1 1
17880057 10.1021/jm070516u Sodium-dependent serotonin transporter 1
17880057 10.1021/jm070516u 5-hydroxytryptamine receptor 7 1
17880057 10.1021/jm070516u 5-hydroxytryptamine receptor 6 1
12565939 10.1016/s0960-894x(02)00996-4 D(2) dopamine receptor 1
17880057 10.1021/jm070516u 5-hydroxytryptamine receptor 2B 1
17880057 10.1021/jm070516u 5-hydroxytryptamine receptor 2A 1
17880057 10.1021/jm070516u 5-hydroxytryptamine receptor 1A 1
17880057 10.1021/jm070516u D(4) dopamine receptor 1
17880057 10.1021/jm070516u D(3) dopamine receptor 1
17880057 10.1021/jm070516u D(2) dopamine receptor 1
12565939 10.1016/s0960-894x(02)00996-4 Sodium-dependent serotonin transporter 1

Data from ChEMBL 36 via Core Engine