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Compound Detail

CHEMBL4869138

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C/C(=N\Nc1nc2ccccc2n1CCN1CCC(F)(F)C1)c1ccccn1

Basic Information

ChEMBL ID CHEMBL4869138
Phase Preclinical
Structure Type MOL
InChI Key VGIXWWLJCGSRBH-MFKUBSTISA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

384.4
MW (Da)
3.61
ALogP
6
HBA
1
HBD
58.3
PSA (Ų)
0.52
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H22F2N6
MW 384.43
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.54

Activity Summary

EC50 3 meas. best 6.92
Kd 1 meas. best 7.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
No relevant target
CHEMBL2362975
Kd 7.58 7.58 26.0 1
Unchecked
CHEMBL612545
EC50 6.92 6.835 120.0 2
TOV112D
CHEMBL3707166
EC50 6.82 6.82 151.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33538587 10.1021/acs.jmedchem.0c01360 Unchecked 5
33538587 10.1021/acs.jmedchem.0c01360 No relevant target 3
33538587 10.1021/acs.jmedchem.0c01360 ADMET 3
33538587 10.1021/acs.jmedchem.0c01360 TOV112D 1
33538587 10.1021/acs.jmedchem.0c01360 NCI-H1299 1
33538587 10.1021/acs.jmedchem.0c01360 Mu-type opioid receptor 1
33538587 10.1021/acs.jmedchem.0c01360 Voltage-gated inwardly rectifying potassium channel KCNH2 1
33538587 10.1021/acs.jmedchem.0c01360 5-hydroxytryptamine receptor 2A 1
33538587 10.1021/acs.jmedchem.0c01360 Sodium-dependent noradrenaline transporter 1

Data from ChEMBL 36 via Core Engine