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Compound Detail

CHEMBL5186271

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[2H]C([2H])([2H])Nc1cc(F)cc2c1[nH]c1nc(Oc3cnc(C)nc3)nc(N3CC(=C(C)C(C)N)C3)c12

Basic Information

ChEMBL ID CHEMBL5186271
Phase Preclinical
Structure Type MOL
InChI Key PAMTZCQKOVUNOU-GKOSEXJESA-N
Parent Compound CHEMBL5172595
Active Moiety CHEMBL5172595
0
Targets
0
Activities
0
Assay Types
10
PK Parameters
6
Publications
0
Known Names

Molecular Properties

448.5
MW (Da)
3.67
ALogP
8
HBA
3
HBD
117.9
PSA (Ų)
0.40
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25FN8O
MW 451.52
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -0.78

Pharmacokinetic Data

Parameter Value Units Species
AUC 696.0 ng.hr.mL-1 Rattus norvegicus
CL 104.0 mL.min-1.g-1 Rattus norvegicus
CL 10.1 mL.min-1.g-1 Homo sapiens
CL 121.0 mL.min-1.kg-1 Rattus norvegicus
F 30.0 % Rattus norvegicus
F 66.0 % Homo sapiens
MRT 5.9 hr Rattus norvegicus
T1/2 0.3367 hr Rattus norvegicus
T1/2 3.467 hr Homo sapiens
T1/2 7.2 hr Rattus norvegicus

Literature References

PubMed DOI Target Context # Activities
34080858 10.1021/acs.jmedchem.1c00621 ADMET 11
34080858 10.1021/acs.jmedchem.1c00621 Escherichia coli 3
34080858 10.1021/acs.jmedchem.1c00621 Klebsiella pneumoniae 3
34080858 10.1021/acs.jmedchem.1c00621 Voltage-gated inwardly rectifying potassium channel KCNH2 2
34080858 10.1021/acs.jmedchem.1c00621 Acinetobacter baumannii 2
34080858 10.1021/acs.jmedchem.1c00621 Pseudomonas aeruginosa 2

Data from ChEMBL 36 via Core Engine