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Compound Detail

CHEMBL5417464

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Cc1cc([C@H]2CN(c3cc(F)c4c(N)nncc4c3)CCN2c2cccc(F)c2)no1

Basic Information

ChEMBL ID CHEMBL5417464
Phase Preclinical
Structure Type MOL
InChI Key HXAFDSAENALNGM-HXUWFJFHSA-N
2
Targets
2
Activities
1
Assay Types
12
PK Parameters
10
Publications
0
Known Names

Molecular Properties

422.4
MW (Da)
3.85
ALogP
7
HBA
1
HBD
84.3
PSA (Ų)
0.54
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H20F2N6O
MW 422.44
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.69

Activity Summary

IC50 2 meas. best 7.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Complement C1s subcomponent
CHEMBL3913
IC50 7.44 7.44 36.0 1
Unchecked
CHEMBL612545
IC50 7.21 7.21 61.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 6017.8 ng.hr.mL-1 Mus musculus
AUC 21928.6 ng.hr.mL-1 Mus musculus
AUC 139341.0 ng.hr.mL-1 Mus musculus
Cmax 2442.95 nM Mus musculus
Cmax 6114.48 nM Mus musculus
Cmax 21058.61 nM Mus musculus
MRT 4.31 hr Mus musculus
MRT 5.02 hr Mus musculus
MRT 7.66 hr Mus musculus
Tmax 1.67 hr Mus musculus
Tmax 2.67 hr Mus musculus
Tmax 4.0 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
37120845 10.1021/acs.jmedchem.3c00348 ADMET 22
37120845 10.1021/acs.jmedchem.3c00348 Unchecked 2
37120845 10.1021/acs.jmedchem.3c00348 Complement C1s subcomponent 1
37120845 10.1021/acs.jmedchem.3c00348 Complement C1r subcomponent 1
37120845 10.1021/acs.jmedchem.3c00348 Mannan-binding lectin serine protease 2 1
37120845 10.1021/acs.jmedchem.3c00348 Complement factor D 1
37120845 10.1021/acs.jmedchem.3c00348 Prothrombin 1
37120845 10.1021/acs.jmedchem.3c00348 Trypsin 1
37120845 10.1021/acs.jmedchem.3c00348 Plasminogen 1
37120845 10.1021/acs.jmedchem.3c00348 Serum 1

Data from ChEMBL 36 via Core Engine