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Compound Detail

CHEMBL5202573

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CN1Cc2nn(Cc3cccc(-c4cccc(C(N)=O)c4)c3)c(-c3ccccc3F)c2C1

Basic Information

ChEMBL ID CHEMBL5202573
Phase Preclinical
Structure Type MOL
InChI Key LGPYOKZMSVIUGM-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
6
PK Parameters
2
Publications
0
Known Names

Molecular Properties

426.5
MW (Da)
4.45
ALogP
4
HBA
1
HBD
64.2
PSA (Ų)
0.51
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H23FN4O
MW 426.50
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.24

Activity Summary

IC50 1 meas. best 7.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.22 7.22 60.5 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 519.57 ng.hr.mL-1 Rattus norvegicus
AUC 341.49 ng.hr.mL-1 Rattus norvegicus
Cmax 351.47 nM Rattus norvegicus
F 16.43 % Rattus norvegicus
T1/2 0.49 hr Rattus norvegicus
T1/2 0.8 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 60.5 nM 7.22 Inhibition of rabbit stomach K+ stimulated H(+)/K(+) ATPase activity incubated f... 35477061

Literature References

PubMed DOI Target Context # Activities
35477061 10.1016/j.bmc.2022.116765 ADMET 6
35477061 10.1016/j.bmc.2022.116765 Unchecked 2

Data from ChEMBL 36 via Core Engine