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Compound Detail

CHEMBL5182845

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Cc1cc(Cl)ccc1-c1ncc(C(=O)N[C@H]2CCc3c(C)ccc(N4CCN(C)CC4)c3C2)cn1

Basic Information

ChEMBL ID CHEMBL5182845
Phase Preclinical
Structure Type MOL
InChI Key GZKULHXXPZXNCM-QFIPXVFZSA-N
1
Targets
2
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

490.1
MW (Da)
4.45
ALogP
5
HBA
1
HBD
61.4
PSA (Ų)
0.59
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H32ClN5O
MW 490.05
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.28

Activity Summary

IC50 2 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.0 5.15 1000.0 2

Pharmacokinetic Data

Parameter Value Units Species
CL 262.0 mL.min-1.g-1 Mus musculus
CL 43.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 1000.0 nM 6.0 Inhibition of Mycobacterium smegmatis ATP synthase 34963068
Unchecked IC50 = 50000.0 nM 4.3 Inhibition of human ATP synthase 34963068

Literature References

PubMed DOI Target Context # Activities
34963068 10.1016/j.ejmech.2021.114059 ADMET 3
34963068 10.1016/j.ejmech.2021.114059 Mycobacterium tuberculosis 2
34963068 10.1016/j.ejmech.2021.114059 Unchecked 2
34963068 10.1016/j.ejmech.2021.114059 Vero 1

Data from ChEMBL 36 via Core Engine