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Compound Detail

CHEMBL1628668

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COc1ccc2c(c1)C(C(=O)N(Cc1ccc(N(C)C)cc1)c1ccc(C(C)C)cc1)CCC2

Basic Information

ChEMBL ID CHEMBL1628668
Phase Preclinical
Structure Type MOL
InChI Key DVYASSBBADJRAS-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
3
PK Parameters
7
Publications
0
Known Names

Molecular Properties

456.6
MW (Da)
6.54
ALogP
3
HBA
0
HBD
32.8
PSA (Ų)
0.40
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H36N2O2
MW 456.63
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.83

Activity Summary

IC50 2 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
C5a anaphylatoxin chemotactic receptor 1
CHEMBL2373
IC50 8.7 8.61 2.0 2

Pharmacokinetic Data

Parameter Value Units Species
F 70.0 % Rattus norvegicus
T1/2 1.0 hr Homo sapiens
T1/2 1.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4495565 SARS-CoV-2 4
28977749 10.1021/acs.jmedchem.7b00882 C5a anaphylatoxin chemotactic receptor 1 2
28977749 10.1021/acs.jmedchem.7b00882 Rattus norvegicus 2
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 2
- 10.6019/CHEMBL4651402 SARS-CoV-2 2
30108770 10.1039/C6MD00581K C5a anaphylatoxin chemotactic receptor 1 1
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1

Data from ChEMBL 36 via Core Engine