Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL4641860

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
COc1c(OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOc2ccc(C3CCN(c4ccn5c(CC6CC6)nnc5c4Cl)CC3)cc2)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1

Basic Information

ChEMBL ID CHEMBL4641860
Phase Preclinical
Structure Type MOL
InChI Key QZSVFPPTVLGYBT-UHFFFAOYSA-N
3
Targets
19
Activities
3
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

1162.8
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C62H85ClFN5O13
MW 1162.83

Activity Summary

IC50 8 meas. best 6.86
Ki 6 meas. best 7.16
EC50 5 meas. best 6.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2A/Metabotropic glutamate receptor 2
CHEMBL4630758
Ki 7.16 7.0375 70.0 4
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 7.1 7.1 79.0 2
5-hydroxytryptamine receptor 2A/Metabotropic glutamate receptor 2
CHEMBL4630758
IC50 6.86 6.4317 138.0 6
5-hydroxytryptamine receptor 2A
CHEMBL224
IC50 6.52 6.52 300.0 2
Metabotropic glutamate receptor 2
CHEMBL5137
EC50 6.5 6.2075 320.0 4
5-hydroxytryptamine receptor 2A/Metabotropic glutamate receptor 2
CHEMBL4630758
EC50 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
5-hydroxytryptamine receptor 2A/Metabotropic glutamate receptor 2 Ki = 70.0 nM 7.16 Displacement of [3H]-ketanserin from human 5HT2A/mGlu2 receptor expressed in HEK... 32815361
5-hydroxytryptamine receptor 2A/Metabotropic glutamate receptor 2 Ki = 72.44 nM 7.14 Displacement of [3H]-ketanserin from human 5HT2A/mGlu2 receptor expressed in HEK... 32815361
5-hydroxytryptamine receptor 2A Ki = 79.43 nM 7.1 Displacement of [3H]-ketanserin from human HT2A receptor expressed in HEK293 cel... 32815361
5-hydroxytryptamine receptor 2A Ki = 79.0 nM 7.1 Displacement of [3H]-ketanserin from human HT2A receptor expressed in HEK293 cel... 32815361
5-hydroxytryptamine receptor 2A/Metabotropic glutamate receptor 2 Ki = 117.49 nM 6.93 Displacement of [3H]-ketanserin from human 5HT2A/mGlu2 receptor expressed in HEK... 32815361
5-hydroxytryptamine receptor 2A/Metabotropic glutamate receptor 2 Ki = 120.0 nM 6.92 Displacement of [3H]-ketanserin from human 5HT2A/mGlu2 receptor expressed in HEK... 32815361
5-hydroxytryptamine receptor 2A/Metabotropic glutamate receptor 2 IC50 = 138.04 nM 6.86 Antagonist activity at human 5HT2A/mGlu2 receptor expressed in HEK293 cells co-e... 32815361
5-hydroxytryptamine receptor 2A/Metabotropic glutamate receptor 2 IC50 = 140.0 nM 6.85 Antagonist activity at human 5HT2A/mGlu2 receptor expressed in HEK293 cells co-e... 32815361
5-hydroxytryptamine receptor 2A/Metabotropic glutamate receptor 2 IC50 = 300.0 nM 6.52 Antagonist activity at human 5HT2A/mGlu2 receptor expressed in HEK293 cells asse... 32815361
5-hydroxytryptamine receptor 2A IC50 = 302.0 nM 6.52 Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed a... 32815361
5-hydroxytryptamine receptor 2A IC50 = 300.0 nM 6.52 Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed a... 32815361
5-hydroxytryptamine receptor 2A/Metabotropic glutamate receptor 2 IC50 = 309.03 nM 6.51 Antagonist activity at human 5HT2A/mGlu2 receptor expressed in HEK293 cells asse... 32815361
Metabotropic glutamate receptor 2 EC50 = 320.0 nM 6.5 Positive modulator activity at human mGlu2 receptor expressed in HEK293 cells co... 32815361
Metabotropic glutamate receptor 2 EC50 = 323.59 nM 6.49 Positive modulator activity at human mGlu2 receptor expressed in HEK293 cells co... 32815361
5-hydroxytryptamine receptor 2A/Metabotropic glutamate receptor 2 IC50 = 1174.9 nM 5.93 Antagonist activity at human 5HT2A/mGlu2 receptor expressed in HEK293 cells co-e... 32815361
5-hydroxytryptamine receptor 2A/Metabotropic glutamate receptor 2 IC50 = 1200.0 nM 5.92 Antagonist activity at human 5HT2A/mGlu2 receptor expressed in HEK293 cells co-e... 32815361
Metabotropic glutamate receptor 2 EC50 = 1202.26 nM 5.92 Agonist activity at human mGlu2 receptor expressed in HEK293 cells co-expressing... 32815361
Metabotropic glutamate receptor 2 EC50 = 1200.0 nM 5.92 Agonist activity at human mGlu2 receptor expressed in HEK293 cells co-expressing... 32815361
5-hydroxytryptamine receptor 2A/Metabotropic glutamate receptor 2 EC50 = 10000.0 nM 5.0 Agonist activity at human 5HT2A/mGlu2 receptor expressed in HEK293 cells co-expr... 32815361

Literature References

PubMed DOI Target Context # Activities
32815361 10.1021/acs.jmedchem.0c01058 5-hydroxytryptamine receptor 2A/Metabotropic glutamate receptor 2 12
32815361 10.1021/acs.jmedchem.0c01058 Metabotropic glutamate receptor 2 6
32815361 10.1021/acs.jmedchem.0c01058 5-hydroxytryptamine receptor 2A 4

Data from ChEMBL 36 via Core Engine