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Compound Detail

CHEMBL1255834

BW-723C86
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CC(N)Cc1c[nH]c2ccc(OCc3cccs3)cc12

Basic Information

ChEMBL ID CHEMBL1255834
Name BW-723C86
Phase Preclinical
Structure Type MOL
InChI Key ALFGDCNSEBJYSP-UHFFFAOYSA-N
12
Targets
30
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

286.4
MW (Da)
3.70
ALogP
3
HBA
2
HBD
51.0
PSA (Ų)
0.75
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C16H18N2OS
MW 286.40
Aromatic Rings 3
Heavy Atoms 20
NP-Likeness -1.17

Activity Summary

IC50 19 meas. best 7.09
Ki 11 meas. best 7.29

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2B
CHEMBL1833
Ki 7.29 7.29 51.6 1
5-hydroxytryptamine receptor 2B
CHEMBL1833
IC50 7.09 7.09 81.1 1
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 6.97 6.97 107.0 1
5-hydroxytryptamine receptor 2C
CHEMBL225
IC50 6.69 6.69 204.3 1
5-hydroxytryptamine receptor 6
CHEMBL3371
Ki 6.53 6.53 297.8 1
5-hydroxytryptamine receptor 1B
CHEMBL3459
Ki 6.4 6.4 400.1 1
5-hydroxytryptamine receptor 1B
CHEMBL3459
IC50 6.38 6.38 421.1 1
5-hydroxytryptamine receptor 6
CHEMBL3371
IC50 6.19 6.19 641.4 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 6.19 6.19 644.5 1
Cytochrome P450 1A2
CHEMBL3356
IC50 6.06 6.06 873.8 1
5-hydroxytryptamine receptor 1A
CHEMBL273
IC50 5.95 5.95 1127.8 1
Unchecked
CHEMBL612545
Ki 5.7 5.53 1983.3 3
Sodium-dependent dopamine transporter
CHEMBL238
Ki 5.67 5.67 2133.0 1
Unchecked
CHEMBL612545
IC50 5.66 5.4933 2173.9 3
Sodium-dependent serotonin transporter
CHEMBL228
Ki 5.59 5.59 2542.0 1
Sodium-dependent dopamine transporter
CHEMBL238
IC50 5.57 5.57 2684.6 1
Cytochrome P450 2D6
CHEMBL289
IC50 5.56 5.56 2774.3 1
Sodium-dependent noradrenaline transporter
CHEMBL222
Ki 5.44 5.44 3595.7 1
Sodium-dependent noradrenaline transporter
CHEMBL222
IC50 5.44 5.44 3625.7 1
Sodium-dependent serotonin transporter
CHEMBL228
IC50 5.32 5.32 4785.0 1
Plasmodium falciparum
CHEMBL364
IC50 5.1 4.9833 7943.3 6

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
5-hydroxytryptamine receptor 2B Ki = 51.6 nM 7.29 DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: ... -
5-hydroxytryptamine receptor 2B IC50 = 81.1 nM 7.09 DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: ... -
5-hydroxytryptamine receptor 2C Ki = 107.0 nM 6.97 DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: ... -
5-hydroxytryptamine receptor 2C IC50 = 204.3 nM 6.69 DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: ... -
5-hydroxytryptamine receptor 6 Ki = 297.8 nM 6.53 DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [... -
5-hydroxytryptamine receptor 1B Ki = 400.1 nM 6.4 DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: ... -
5-hydroxytryptamine receptor 1B IC50 = 421.1 nM 6.38 DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: ... -
5-hydroxytryptamine receptor 1A Ki = 644.5 nM 6.19 DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: ... -
5-hydroxytryptamine receptor 6 IC50 = 641.4 nM 6.19 DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [... -
Cytochrome P450 1A2 IC50 = 873.8 nM 6.06 DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) -
5-hydroxytryptamine receptor 1A IC50 = 1127.8 nM 5.95 DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: ... -
Unchecked Ki = 1983.3 nM 5.7 DRUGMATRIX: Sodium Channel, Site 2 radioligand binding (ligand: [3H] Batrachotox... -
Sodium-dependent dopamine transporter Ki = 2133.0 nM 5.67 DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) -
Unchecked IC50 = 2173.9 nM 5.66 DRUGMATRIX: Sodium Channel, Site 2 radioligand binding (ligand: [3H] Batrachotox... -
Sodium-dependent serotonin transporter Ki = 2542.0 nM 5.59 DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand bind... -
Sodium-dependent dopamine transporter IC50 = 2684.6 nM 5.57 DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) -
Cytochrome P450 2D6 IC50 = 2774.3 nM 5.56 DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) -
Unchecked Ki = 3084.1 nM 5.51 DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand:... -
Unchecked IC50 = 3469.6 nM 5.46 DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand:... -
Sodium-dependent noradrenaline transporter IC50 = 3625.7 nM 5.44 DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-5... -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3885881 Rattus norvegicus 207
19734910 10.1038/nchembio.215 Plasmodium falciparum 6
17417631 10.1038/nchembio873 Unchecked 1
- 10.6019/CHEMBL3301361 No relevant target 1

Data from ChEMBL 36 via Core Engine