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Compound Detail

CHEMBL4093031

BMS-929075
Phase I
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Phase I
CNC(=O)c1c(-c2ccc(F)cc2)oc2ccc(-c3cc(C(=O)NC4(c5ncccn5)CC4)ccc3C)c(F)c12

Basic Information

ChEMBL ID CHEMBL4093031
Name BMS-929075
Phase Phase I
Structure Type MOL
InChI Key LZAUGCMVNLZVJV-UHFFFAOYSA-N

Known Names

Bms-929075
4
Targets
12
Activities
2
Assay Types
14
PK Parameters
18
Publications
1
Known Names
1
Indications

Molecular Properties

538.5
MW (Da)
5.92
ALogP
5
HBA
2
HBD
97.1
PSA (Ų)
0.28
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral

Extended Properties

Molecular Formula C31H24F2N4O3
MW 538.55
Aromatic Rings 5
Heavy Atoms 40
NP-Likeness -0.73

Indications

Hepatitis C, Chronic

Activity Summary

EC50 9 meas. best 8.7
IC50 3 meas. best 5.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hepatitis C virus
CHEMBL379
EC50 8.7 7.8613 2.0 8
Unchecked
CHEMBL612545
EC50 7.75 7.75 18.0 1
Cytochrome P450 2C8
CHEMBL3721
IC50 5.17 5.17 6700.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 4.75 4.685 18000.0 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 75504.71 ng.hr.mL-1 Rattus norvegicus
AUC 29350.97 ng.hr.mL-1 Rattus norvegicus
CL 1.7 mL.min-1.kg-1 Rattus norvegicus
Cmax 14700.0 nM Rattus norvegicus
Cmax 7500.0 nM Rattus norvegicus
F 48.0 % Rattus norvegicus
F 100.0 % Rattus norvegicus
T1/2 2.0 hr Macaca mulatta
T1/2 2.0 hr Canis lupus familiaris
T1/2 2.0 hr Rattus norvegicus
T1/2 2.0 hr Homo sapiens
T1/2 4.7 hr Rattus norvegicus
Tmax 4.0 hr Rattus norvegicus
Tmax 4.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Hepatitis C virus EC50 = 2.0 nM 8.7 Antiviral activity against HCV genotype 5a infected in human HuH7 cells after 3 ... 28430437
Hepatitis C virus EC50 = 3.0 nM 8.52 Antiviral activity against HCV genotype 4a infected in human HuH7 cells after 3 ... 28430437
Hepatitis C virus EC50 = 4.0 nM 8.4 Antiviral activity against HCV genotype 1a infected in human HuH7 cells after 3 ... 28430437
Hepatitis C virus EC50 = 5.0 nM 8.3 Antiviral activity against HCV genotype 6a infected in human HuH7 cells after 3 ... 28430437
Hepatitis C virus EC50 = 9.0 nM 8.05 Antiviral activity against HCV genotype 1b infected in human HuH7 cells after 3 ... 28430437
Unchecked EC50 = 18.0 nM 7.75 Inhibition of HCV genotype 1b NS5B replicase C316N mutant infected in human HuH7... 28430437
Hepatitis C virus EC50 = 22.0 nM 7.66 Antiviral activity against HCV genotype 3a infected in human HuH7 cells after 3 ... 28430437
Hepatitis C virus EC50 = 115.0 nM 6.94 Antiviral activity against HCV genotype 2b infected in human HuH7 cells after 3 ... 28430437
Hepatitis C virus EC50 = 481.0 nM 6.32 Antiviral activity against HCV genotype 2a infected in human HuH7 cells after 3 ... 28430437
Cytochrome P450 2C8 IC50 = 6700.0 nM 5.17 Inhibition of microsomal CYP2C8 (unknown origin) 28430437
Voltage-gated inwardly rectifying potassium channel KCNH2 IC50 = 18000.0 nM 4.75 Inhibition of human ERG by patch clamp assay 28430437
Voltage-gated inwardly rectifying potassium channel KCNH2 IC50 = 24000.0 nM 4.62 Inhibition of human ERG by thallium flux assay 28430437

Literature References

PubMed DOI Target Context # Activities
28430437 10.1021/acs.jmedchem.7b00328 Hepatitis C virus 12
28430437 10.1021/acs.jmedchem.7b00328 Rattus norvegicus 12
28430437 10.1021/acs.jmedchem.7b00328 Liver 5
28430437 10.1021/acs.jmedchem.7b00328 No relevant target 4
28430437 10.1021/acs.jmedchem.7b00328 Serum 4
28430437 10.1021/acs.jmedchem.7b00328 Unchecked 3
28430437 10.1021/acs.jmedchem.7b00328 ADMET 3
28430437 10.1021/acs.jmedchem.7b00328 Voltage-gated inwardly rectifying potassium channel KCNH2 3
28430437 10.1021/acs.jmedchem.7b00328 Homo sapiens 2
28430437 10.1021/acs.jmedchem.7b00328 Sodium channel protein type 5 subunit alpha 1
28430437 10.1021/acs.jmedchem.7b00328 Nuclear receptor subfamily 1 group I member 2 1
28430437 10.1021/acs.jmedchem.7b00328 Voltage-dependent L-type calcium channel subunit alpha-1C 1
28430437 10.1021/acs.jmedchem.7b00328 Cytochrome P450 3A4 1
28430437 10.1021/acs.jmedchem.7b00328 Cytochrome P450 2C8 1
28430437 10.1021/acs.jmedchem.7b00328 Huh-7 1
28430437 10.1021/acs.jmedchem.7b00328 HepG2 1
28430437 10.1021/acs.jmedchem.7b00328 Hepatocyte 1
28430437 10.1021/acs.jmedchem.7b00328 Canis familiaris 1

Data from ChEMBL 36 via Core Engine