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Compound Detail

CHEMBL3360975

BMS-779788
Phase I
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Phase I
CC(C)(O)c1cn(-c2ccc(-c3cccc(S(C)(=O)=O)c3)cc2)c(C(C)(C)c2ccccc2Cl)n1

Basic Information

ChEMBL ID CHEMBL3360975
Name BMS-779788
Phase Phase I
Structure Type MOL
InChI Key JLPURTXCSILYLW-UHFFFAOYSA-N

Known Names

BMS 788 Bms-779788 EXEL 04286652 EXEL-04286652 XL 652 XL-014 XL-652
6
Targets
20
Activities
2
Assay Types
7
PK Parameters
20
Publications
7
Known Names
1
Indications
1
Mechanisms

Molecular Properties

509.1
MW (Da)
6.15
ALogP
5
HBA
1
HBD
72.2
PSA (Ų)
0.34
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral

Extended Properties

Molecular Formula C28H29ClN2O3S
MW 509.07
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.10

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
LXR-beta agonist AGONIST Oxysterols receptor LXR-beta

Indications

Atherosclerosis

Activity Summary

EC50 16 meas. best 8.92
Ki 4 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Liver X receptor
CHEMBL3706564
EC50 8.92 8.2 1.2 2
Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-beta
CHEMBL3430878
Ki 7.85 7.85 14.0 2
Oxysterols receptor LXR-beta
CHEMBL4093
EC50 7.48 6.435 33.0 8
Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha
CHEMBL3430879
Ki 7.17 7.17 68.0 2
Oxysterols receptor LXR-alpha
CHEMBL2808
EC50 6.7 6.504 200.0 5
Cynomolgus monkey
CHEMBL613847
EC50 6.21 6.21 610.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 1.9 mL.min-1.kg-1 Macaca fascicularis
CL 2.9 mL.min-1.kg-1 Macaca fascicularis
Cmax 2227.0 nM Macaca fascicularis
T1/2 7.4 hr Macaca fascicularis
T1/2 8.9 hr Macaca fascicularis
T1/2 100.0 hr Homo sapiens
Tmax 2.0 hr Macaca fascicularis

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Liver X receptor EC50 = 1.2 nM 8.92 Transactivation of LXR in human whole blood assessed as induction of ABCA1 after... 25435151
Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-beta Ki = 14.0 nM 7.85 Displacement of [3H]-24,25-epoxycholesterol from human LXRbeta/RXRalpha expresse... 27994765
Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-beta Ki = 14.0 nM 7.85 Binding affinity to LXRbeta-RXRalpha heterodimer (unknown origin) expressed in i... 25435151
Liver X receptor EC50 = 33.0 nM 7.48 Transactivation of LXR (unknown origin) expressed in human HeLa cells by ABCA1 L... 25435151
Oxysterols receptor LXR-beta EC50 = 33.0 nM 7.48 Agonist activity at LXR-beta in human HeLa cells assessed as induction of ABCA1 ... 27994765
Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha Ki = 68.0 nM 7.17 Displacement of [3H]-24,25-epoxycholesterol from human LXRalpha/RXRalpha express... 27994765
Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha Ki = 68.0 nM 7.17 Binding affinity to LXRalpha-RXRalpha heterodimer (unknown origin) expressed in ... 25435151
Oxysterols receptor LXR-alpha EC50 = 200.0 nM 6.7 Affinity On-target Cellular interaction: (Reporter gene assay (HEK293T cells)) E... -
Oxysterols receptor LXR-alpha EC50 = 220.0 nM 6.66 Agonist activity at human LXR-alpha expressed in African green monkey CV1 cells ... 27994765
Oxysterols receptor LXR-alpha EC50 = 230.0 nM 6.64 Transactivation of LXRalpha (unknown origin) expressed in CV1 cells by luciferas... 25435151
Oxysterols receptor LXR-beta EC50 = 250.0 nM 6.6 Agonist activity at human LXR-beta expressed in African green monkey CV1 cells m... 27994765
Oxysterols receptor LXR-beta EC50 = 250.0 nM 6.6 Transactivation of LXRbeta (unknown origin) expressed in CV1 cells by luciferase... 25435151
Oxysterols receptor LXR-beta EC50 = 300.0 nM 6.52 Affinity On-target Cellular interaction: (Reporter gene assay (HEK293T cells)) E... -
Oxysterols receptor LXR-alpha EC50 = 550.0 nM 6.26 ligand sensing assay (LiSA): As used herein, reference to the activity of an LXR... -
Oxysterols receptor LXR-alpha EC50 = 550.0 nM 6.26 ligand sensing assay (LiSA): As used herein, reference to the activity of an LXR... -
Cynomolgus monkey EC50 = 610.0 nM 6.21 In vivo transactivation in po dosed cynomolgus monkey blood assessed as inductio... 30004226
Oxysterols receptor LXR-beta EC50 = 630.0 nM 6.2 ligand sensing assay (LiSA): As used herein, reference to the activity of an LXR... -
Oxysterols receptor LXR-beta EC50 = 630.0 nM 6.2 ligand sensing assay (LiSA): As used herein, reference to the activity of an LXR... -
Oxysterols receptor LXR-beta EC50 = 1100.0 nM 5.96 Agonist activity at LXR-beta in human whole blood assessed as ABCG1 gene inducti... 27994765
Oxysterols receptor LXR-beta EC50 = 1200.0 nM 5.92 Agonist activity at LXR-beta in human whole blood assessed as ABCA1 gene inducti... 27994765

Literature References

PubMed DOI Target Context # Activities
25435151 10.1016/j.bmcl.2014.11.029 Mus musculus 10
27994765 10.1021/acsmedchemlett.6b00234 Oxysterols receptor LXR-beta 8
- 10.6019/CHEMBL5303304 Fibroblast 8
- 10.6019/CHEMBL5303304 HEK-293T 8
30004226 10.1021/acs.jmedchem.8b00045 Cynomolgus monkey 6
25435151 10.1016/j.bmcl.2014.11.029 Plasma 5
27994765 10.1021/acsmedchemlett.6b00234 ADMET 5
- 10.6019/CHEMBL5303304 U2OS 5
25435151 10.1016/j.bmcl.2014.11.029 Liver X receptor 4
- 10.6019/CHEMBL5724696 TERT-RPE1 4
25435151 10.1016/j.bmcl.2014.11.029 Oxysterols receptor LXR-alpha 2
25435151 10.1016/j.bmcl.2014.11.029 Oxysterols receptor LXR-beta 2
27994765 10.1021/acsmedchemlett.6b00234 Oxysterols receptor LXR-alpha 2
27994765 10.1021/acsmedchemlett.6b00234 Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha 1
27994765 10.1021/acsmedchemlett.6b00234 Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-beta 1
27994765 10.1021/acsmedchemlett.6b00234 Alpha-1-acid glycoprotein 1 1
27994765 10.1021/acsmedchemlett.6b00234 Albumin 1
27994765 10.1021/acsmedchemlett.6b00234 Alpha-1-acid glycoprotein 1
25435151 10.1016/j.bmcl.2014.11.029 Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha 1
25435151 10.1016/j.bmcl.2014.11.029 Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-beta 1

Data from ChEMBL 36 via Core Engine