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Compound Detail

CHEMBL3893594

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COc1ccc(NC(=O)C2=C(c3ccc(C)cc3)C[C@](c3ccc(OCCCC(F)(F)F)cc3)(C(F)(F)F)NC2=O)cc1

Basic Information

ChEMBL ID CHEMBL3893594
Phase Preclinical
Structure Type MOL
InChI Key FBBPRPJENPWDPL-LJAQVGFWSA-N
3
Targets
7
Activities
1
Assay Types
6
PK Parameters
7
Publications
0
Known Names

Molecular Properties

606.6
MW (Da)
7.09
ALogP
4
HBA
2
HBD
76.7
PSA (Ų)
0.15
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H28F6N2O4
MW 606.56
Aromatic Rings 3
Heavy Atoms 43
NP-Likeness -0.58

Activity Summary

IC50 7 meas. best 9.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase
CHEMBL2375203
IC50 9.24 8.69 0.6 2
Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase
CHEMBL2321630
IC50 9.2 8.5975 0.6 4
Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase
CHEMBL4879456
IC50 8.51 8.51 3.1 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1.1 uM Mus musculus
Cmax 160.0 nM Mus musculus
F 15.0 % Mus musculus
Fu 0.008 - Homo sapiens
Fu 0.024 - Rattus norvegicus
Fu 0.014 - Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34613725 10.1021/acs.jmedchem.1c01356 ADMET 11
34613725 10.1021/acs.jmedchem.1c01356 Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase 5
34613725 10.1021/acs.jmedchem.1c01356 Mus musculus 5
34613725 10.1021/acs.jmedchem.1c01356 No relevant target 3
34613725 10.1021/acs.jmedchem.1c01356 Beta-1,4-mannosyl-glycoprotein 4-beta-N-acetylglucosaminyltransferase 1
34613725 10.1021/acs.jmedchem.1c01356 Acyl-CoA wax alcohol acyltransferase 2 1
34613725 10.1021/acs.jmedchem.1c01356 Diacylglycerol O-acyltransferase 1 1

Data from ChEMBL 36 via Core Engine