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Compound Detail

CHEMBL4297354

AZD-7687
Phase I
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Phase I
Cc1nc(C)c(-c2ccc(C3CCC(CC(=O)O)CC3)cc2)nc1C(N)=O
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL4297354
Name AZD-7687
Phase Phase I
Structure Type MOL
InChI Key YXFNPRHZMOGREC-UHFFFAOYSA-N

Known Names

Azd 7687 Azd-7687 Azd7687
11
Targets
16
Activities
2
Assay Types
22
PK Parameters
20
Publications
3
Known Names
1
Indications
1
Mechanisms

Molecular Properties

367.4
MW (Da)
3.61
ALogP
4
HBA
2
HBD
106.2
PSA (Ų)
0.84
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Racemic

Extended Properties

Molecular Formula C21H25N3O3
MW 367.45
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.31

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Diacylglycerol O-acyltransferase 1 inhibitor INHIBITOR Diacylglycerol O-acyltransferase 1 ✓ ✓

Indications

Obesity

Activity Summary

IC50 15 meas. best 8.0
EC50 1 meas. best 6.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Diacylglycerol O-acyltransferase 1
CHEMBL6009
 IC50 8.0 7.565 10.0 4
Rattus norvegicus
CHEMBL376
 IC50 7.38 7.13 42.0 2
O-acyltransferase
CHEMBL2176848
 IC50 7.22 7.22 60.0 1
Diacylglycerol O-acyltransferase 2
CHEMBL5853
 IC50 7.1 7.1 80.0 1
Diacylglycerol O-acyltransferase 1
CHEMBL6129
 IC50 7.05 6.935 90.0 2
Diacylglycerol O-acyltransferase 1
CHEMBL1075284
 IC50 7.0 7.0 100.0 1
Homo sapiens
CHEMBL372
 EC50 6.36 6.36 440.0 1
Fatty-acid amide hydrolase 1
CHEMBL2243
 IC50 5.43 5.43 3700.0 1
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
CHEMBL4409
 IC50 5.26 5.26 5500.0 1
Sterol O-acyltransferase 1
CHEMBL2782
 IC50 4.47 4.47 34000.0 1
Muscarinic acetylcholine receptor M2
CHEMBL211
 IC50 4.09 4.09 80500.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 1.2 mL.min-1.kg-1 Canis lupus familiaris
CL 0.5 mL.min-1.kg-1 Rattus norvegicus
CL 0.77 mL.min-1.kg-1 Mus musculus
F 100.0 % Canis lupus familiaris
F 100.0 % Mus musculus
F 93.0 % Rattus norvegicus
Fu 0.06 - Canis lupus familiaris
Fu 0.1 - Mus musculus
Fu 0.03 - Rattus norvegicus
Fu 0.047 - Homo sapiens
T1/2 9.0 hr Homo sapiens
T1/2 11.0 hr Canis lupus familiaris
T1/2 13.0 hr Mus musculus
T1/2 7.6 hr -
T1/2 2400.0 hr -
T1/2 14.0 hr Rattus norvegicus
T1/2 9.0 hr Homo sapiens
Tmax 1.0 hr Homo sapiens
Tmax 1.0 hr Homo sapiens
Vd 1.0 L.kg-1 Canis lupus familiaris
Vd 0.35 L.kg-1 Rattus norvegicus
Vd 0.9 L.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Diacylglycerol O-acyltransferase 1 IC50 = 10.0 nM 8.0 Inhibition of DGAT1 in human HuTu80 cells 23116186
Diacylglycerol O-acyltransferase 1 IC50 = 10.0 nM 8.0 Inhibition of DGAT1 in human adipose tissue assessed as reduction in triacylglyc... 23116186
Rattus norvegicus IC50 = 42.0 nM 7.38 Inhibition of plasma triacylglycerol excursion in 14 hrs fasted Han-Wistar rat a... 23116186
O-acyltransferase IC50 = 60.0 nM 7.22 Inhibition of DGAT1 in dog liver microsomes 23116186
Diacylglycerol O-acyltransferase 1 IC50 = 70.0 nM 7.16 Inhibition of DGAT1 in human liver microsomes 23116186
Diacylglycerol O-acyltransferase 1 IC50 = 80.0 nM 7.1 Inhibition of human recombinant DGAT1 expressed in Sf9 cells by liquid scintillo... 23116186
Diacylglycerol O-acyltransferase 2 IC50 = 80.0 nM 7.1 Inhibition of recombinant FLAG-tagged human DGAT2 expressed in SF9 cells after 1... 31930920
Diacylglycerol O-acyltransferase 1 IC50 = 90.0 nM 7.05 Inhibition of DGAT1 in rat adipose tissue assessed as reduction in triacylglycer... 23116186
Diacylglycerol O-acyltransferase 1 IC50 = 100.0 nM 7.0 Inhibition of DGAT1 in mouse liver microsomes 23116186
Rattus norvegicus IC50 = 132.0 nM 6.88 Inhibition of adipose triacylglycerol synthesis in 14 hrs fasted Han-Wistar rat ... 23116186
Diacylglycerol O-acyltransferase 1 IC50 = 150.0 nM 6.82 Inhibition of DGAT1 in rat liver microsomes 23116186
Homo sapiens EC50 = 440.0 nM 6.36 Reduction of triglyceride AUC in human 23919406
Fatty-acid amide hydrolase 1 IC50 = 3700.0 nM 5.43 Inhibition of FAAH 23116186
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A IC50 = 5500.0 nM 5.26 Inhibition of PDE10A1 receptor 23116186
Sterol O-acyltransferase 1 IC50 = 34000.0 nM 4.47 Inhibition of human ACAT1 by liquid scintillography 23116186
Muscarinic acetylcholine receptor M2 IC50 = 80500.0 nM 4.09 Inhibition of muscarinic M2 receptor 23116186

Literature References

PubMed DOI Target Context # Activities
23116186 10.1021/jm301296t Rattus norvegicus 8
23116186 10.1021/jm301296t Diacylglycerol O-acyltransferase 1 7
23919406 10.1021/jm4007033 Homo sapiens 6
23116186 10.1021/jm301296t Canis familiaris 4
23116186 10.1021/jm301296t Mus musculus 4
23116186 10.1021/jm301296t No relevant target 4
23116186 10.1021/jm301296t Plasma 4
23116186 10.1021/jm301296t Homo sapiens 3
23116186 10.1021/jm301296t Hepatocyte 3
23116186 10.1021/jm301296t Sterol O-acyltransferase 1 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
23116186 10.1021/jm301296t Cytochrome P450 2D6 1
23116186 10.1021/jm301296t cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A 1
23116186 10.1021/jm301296t Voltage-gated inwardly rectifying potassium channel KCNH2 1
23116186 10.1021/jm301296t Cytochrome P450 2C9 1
23116186 10.1021/jm301296t Cytochrome P450 2C19 1
23116186 10.1021/jm301296t Muscarinic acetylcholine receptor M2 1
23116186 10.1021/jm301296t Cytochrome P450 3A4 1
23116186 10.1021/jm301296t ADMET 1

Data from ChEMBL 36 via Core Engine