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Compound Detail

CHEMBL4102031

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CC(C)C[C@H](NC(=O)c1cnn(-c2ccc(F)cc2)n1)C(=O)NC1(C#N)CC1

Basic Information

ChEMBL ID CHEMBL4102031
Phase Preclinical
Structure Type MOL
InChI Key MRGWDCFIRKJQCI-HNNXBMFYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

384.4
MW (Da)
1.72
ALogP
6
HBA
2
HBD
112.7
PSA (Ų)
0.75
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H21FN6O2
MW 384.42
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -1.58

Activity Summary

IC50 1 meas. best 5.66
Ki 1 meas. best 7.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rhodesain
CHEMBL4188
Ki 7.64 7.64 23.0 1
Trypanosoma brucei rhodesiense
CHEMBL612348
IC50 5.66 5.66 2200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29590751 10.1021/acs.jmedchem.7b01870 No relevant target 2
29590751 10.1021/acs.jmedchem.7b01870 Rhodesain 1
29590751 10.1021/acs.jmedchem.7b01870 Unchecked 1
29590751 10.1021/acs.jmedchem.7b01870 Trypanosoma brucei rhodesiense 1

Data from ChEMBL 36 via Core Engine