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Compound Detail

CHEMBL4578164

MRL-CB1-NC
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CC(=O)c1c(NS(C)(=O)=O)c2cc(-c3ccc(Cl)cc3)c(-c3ccc(Cl)cc3Cl)nc2n(C)c1=O

Basic Information

ChEMBL ID CHEMBL4578164
Name MRL-CB1-NC
Phase Preclinical
Structure Type MOL
InChI Key HSEQWGUPLOFKEC-UHFFFAOYSA-N
10
Targets
24
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

550.9
MW (Da)
5.80
ALogP
6
HBA
1
HBD
98.1
PSA (Ų)
0.32
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H18Cl3N3O4S
MW 550.85
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.02

Activity Summary

Ki 23 meas. best 7.7
IC50 1 meas. best 7.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 7.7 7.6733 19.9 3
Cannabinoid receptor 1
CHEMBL218
IC50 7.49 7.49 32.5 1
Sodium-dependent dopamine transporter
CHEMBL238
Ki 6.12 6.1133 766.0 3
Beta-3 adrenergic receptor
CHEMBL246
Ki 5.95 5.9333 1134.0 3
Delta-type opioid receptor
CHEMBL236
Ki 5.85 5.85 1412.5 3
GABA-A receptor; anion channel
CHEMBL1907607
Ki 5.78 5.78 1659.6 2
Gamma-aminobutyric acid receptor subunit alpha-1
CHEMBL1962
Ki 5.78 5.78 1666.0 1
Alpha-2B adrenergic receptor
CHEMBL1942
Ki 5.77 5.77 1694.0 3
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 5.74 5.74 1815.0 3
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 5.0 5.0 10000.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
5-hydroxytryptamine receptor 2C Ki = 19.95 nM 7.7 GPCRScan assay: inhibition of 5-HT2C -
5-hydroxytryptamine receptor 2C Ki = 22.0 nM 7.66 GPCRScan assay: inhibition of 5-HT2C -
5-hydroxytryptamine receptor 2C Ki = 22.0 nM 7.66 Selectivity interaction (GPCR panel (PDSP screen)) EUB0000316b HTR2C -
Cannabinoid receptor 1 IC50 = 32.5 nM 7.49 Affinity Biochemical interaction (Radioligand binding assay (CNR1, inverse agoni... -
Sodium-dependent dopamine transporter Ki = 766.0 nM 6.12 GPCRScan assay: inhibition of DAT -
Sodium-dependent dopamine transporter Ki = 766.0 nM 6.12 Selectivity interaction (GPCR panel (PDSP screen)) EUB0000316b SLC6A3 -
Sodium-dependent dopamine transporter Ki = 794.33 nM 6.1 GPCRScan assay: inhibition of DAT -
Beta-3 adrenergic receptor Ki = 1134.0 nM 5.95 GPCRScan assay: inhibition of Beta3 -
Beta-3 adrenergic receptor Ki = 1134.0 nM 5.95 Selectivity interaction (GPCR panel (PDSP screen)) EUB0000316b ADRB3 -
Beta-3 adrenergic receptor Ki = 1258.93 nM 5.9 GPCRScan assay: inhibition of Beta3 -
Delta-type opioid receptor Ki = 1415.0 nM 5.85 Selectivity interaction (GPCR panel (PDSP screen)) EUB0000316b OPRD1 -
Delta-type opioid receptor Ki = 1412.54 nM 5.85 GPCRScan assay: inhibition of DOR -
Delta-type opioid receptor Ki = 1415.0 nM 5.85 GPCRScan assay: inhibition of DOR -
GABA-A receptor; anion channel Ki = 1660.0 nM 5.78 GPCRScan assay: inhibition of GABAA/BZP -
GABA-A receptor; anion channel Ki = 1659.59 nM 5.78 GPCRScan assay: inhibition of GABAA/BZP -
Gamma-aminobutyric acid receptor subunit alpha-1 Ki = 1666.0 nM 5.78 Selectivity interaction (GPCR panel (PDSP screen)) EUB0000316b GABRA1 -
Alpha-2B adrenergic receptor Ki = 1694.0 nM 5.77 GPCRScan assay: inhibition of Alpha2B -
Alpha-2B adrenergic receptor Ki = 1698.24 nM 5.77 GPCRScan assay: inhibition of Alpha2B -
Alpha-2B adrenergic receptor Ki = 1694.0 nM 5.77 Selectivity interaction (GPCR panel (PDSP screen)) EUB0000316b ADRA2B -
5-hydroxytryptamine receptor 2A Ki = 1815.0 nM 5.74 GPCRScan assay: inhibition of 5-HT2A -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4507287 Tyrosine-protein kinase ABL1 15
- 10.6019/CHEMBL5674860 Colon cancer organoid 12
- 10.6019/CHEMBL5724558 Colon cancer organoid 12
- 10.6019/CHEMBL4507287 Epidermal growth factor receptor 12
- 10.6019/CHEMBL4507287 Receptor-type tyrosine-protein kinase FLT3 11
- 10.6019/CHEMBL4689842 Fibroblast 10
- 10.6019/CHEMBL4507287 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 10
- 10.6019/CHEMBL4689842 HEK-293T 10
- 10.6019/CHEMBL4689842 U2OS 9
- 10.6019/CHEMBL4507287 Mast/stem cell growth factor receptor Kit 9
- 10.6019/CHEMBL4507287 Unchecked 8
- 10.6019/CHEMBL5608141 Colon cancer organoid 6
- 10.1158/2159-8290.CD-23-0050 Colon cancer organoid 5
- 10.6019/CHEMBL4507287 Proto-oncogene tyrosine-protein kinase receptor Ret 4
- 10.6019/CHEMBL4507287 GABA-A receptor; anion channel 4
- 10.6019/CHEMBL4507287 Alpha-2C adrenergic receptor 3
- 10.6019/CHEMBL4507287 Alpha-2B adrenergic receptor 3
- 10.6019/CHEMBL4507287 Beta-3 adrenergic receptor 3
- 10.6019/CHEMBL4507287 ALK tyrosine kinase receptor 3
- 10.6019/CHEMBL4507287 5-hydroxytryptamine receptor 2C 3

Data from ChEMBL 36 via Core Engine