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Compound Detail

CHEMBL85156

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C=CCNc1nc(NCC=C)nc(N2CCC(NCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)n1

Basic Information

ChEMBL ID CHEMBL85156
Phase Preclinical
Structure Type MOL
InChI Key GERNFWKTMKWULM-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

505.6
MW (Da)
4.74
ALogP
7
HBA
3
HBD
78.0
PSA (Ų)
0.31
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H33F2N7
MW 505.62
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -0.97

Activity Summary

Ki 1 meas. best 7.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Voltage-dependent L-type calcium channel subunit alpha-1S
CHEMBL4108
Ki 7.05 7.05 89.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
1352353 10.1021/jm00091a017 DC3F/AD 6
1352353 10.1021/jm00091a017 KB 3
8831775 10.1021/jm960361i P388 2
8831775 10.1021/jm960361i KB 2
1352353 10.1021/jm00091a017 P388/VCR 2
1352353 10.1021/jm00091a017 P388 2
- 10.6019/CHEMBL4651402 SARS-CoV-2 2
8831775 10.1021/jm960361i Voltage-dependent L-type calcium channel subunit alpha-1S 1
8831775 10.1021/jm960361i Mus musculus 1
15180340 10.1023/b:pham.0000026434.82855.69 ATP-dependent translocase ABCB1 1
9205004 10.1038/sj.leu.2400698 ATP-dependent translocase ABCB1 1

Data from ChEMBL 36 via Core Engine