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Compound Detail

CHEMBL4103808

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Cc1cc(Oc2ccc(-c3ccn4c(CC5CC5)nnc4c3C(F)(F)F)cc2F)ccn1

Basic Information

ChEMBL ID CHEMBL4103808
Phase Preclinical
Structure Type MOL
InChI Key RJDUDNJPUMXPBA-UHFFFAOYSA-N
1
Targets
3
Activities
3
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

442.4
MW (Da)
6.00
ALogP
5
HBA
0
HBD
52.3
PSA (Ų)
0.36
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H18F4N4O
MW 442.42
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.08

Activity Summary

EC50 1 meas. best 7.25
Kd 1 meas. best 8.04
Ki 1 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Metabotropic glutamate receptor 2
CHEMBL5137
Ki 8.15 8.15 7.1 1
Metabotropic glutamate receptor 2
CHEMBL5137
Kd 8.04 8.04 9.2 1
Metabotropic glutamate receptor 2
CHEMBL5137
EC50 7.25 7.25 56.2 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28704052 10.1021/acs.jmedchem.7b00669 Metabotropic glutamate receptor 2 6

Data from ChEMBL 36 via Core Engine