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Compound Detail

CHEMBL4060400

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Cc1nn2c(O)cc(C3CCN(C(=O)OCc4ccccc4)CC3)nc2c1-c1ccc(F)cc1

Basic Information

ChEMBL ID CHEMBL4060400
Phase Preclinical
Structure Type MOL
InChI Key DQKIDQKOAUUVAT-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

460.5
MW (Da)
5.07
ALogP
6
HBA
1
HBD
80.0
PSA (Ų)
0.46
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H25FN4O3
MW 460.51
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.45

Activity Summary

EC50 4 meas. best 6.63

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Short transient receptor potential channel 3
CHEMBL2417348
EC50 6.63 6.63 236.0 1
Short transient receptor potential channel 7
CHEMBL4105799
EC50 6.5 6.5 314.0 1
Short transient receptor potential channel 6
CHEMBL1795081
EC50 5.49 5.45 3240.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28395140 10.1021/acs.jmedchem.7b00304 Short transient receptor potential channel 4 4
28395140 10.1021/acs.jmedchem.7b00304 Short transient receptor potential channel 6 3
28395140 10.1021/acs.jmedchem.7b00304 Short transient receptor potential channel 3 3
28395140 10.1021/acs.jmedchem.7b00304 Transient receptor potential cation channel subfamily M member 8 2
28395140 10.1021/acs.jmedchem.7b00304 Unchecked 2
28395140 10.1021/acs.jmedchem.7b00304 Short transient receptor potential channel 7 1
28395140 10.1021/acs.jmedchem.7b00304 Short transient receptor potential channel 5 1
28395140 10.1021/acs.jmedchem.7b00304 Transient receptor potential cation channel subfamily A member 1 1
28395140 10.1021/acs.jmedchem.7b00304 Transient receptor potential cation channel subfamily V member 1 1
28395140 10.1021/acs.jmedchem.7b00304 Transient receptor potential cation channel subfamily V member 3 1
28395140 10.1021/acs.jmedchem.7b00304 Transient receptor potential cation channel subfamily V member 4 1
28395140 10.1021/acs.jmedchem.7b00304 Transient receptor potential cation channel subfamily M member 5 1

Data from ChEMBL 36 via Core Engine