Compound Detail

CHEMBL4558527

AZD-8154

🧪 Phase II

Enter ChEMBL ID:

Free Research Context This compound will appear in recent viewed items on the research home for this browser.

Research home View demo workspace

🧪 Phase II

Cc1nc(Nc2cccc(N3CCCC3=O)n2)sc1-c1cc2c(c(S(C)(=O)=O)c1)C(=O)N([C@@H](C)C1CC1)C2

ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID	CHEMBL4558527
Name	AZD-8154
Phase	Phase II
Structure Type	MOL
InChI Key	XOMFDZJQLSPGGV-INIZCTEOSA-N

Known Names

Azd 8154 Azd-8154 AZD8154

Targets

Activities

Assay Types

PK Parameters

Publications

Known Names

Indications

Molecular Properties

551.7

MW (Da)

4.54

ALogP

HBA

HBD

112.6

PSA (Å²)

0.46

QED

Ro5 Violations

Rot. Bonds

Drug Information

Molecule Type	Small molecule
Chirality	Single Enantiomer

Extended Properties

Molecular Formula	C27H29N5O4S2
MW	551.69
Aromatic Rings	3
Heavy Atoms	38
NP-Likeness	-1.34

Indications

Asthma

Activity Summary

IC50 10 meas. best 9.2

Target Activity Profile

Target	Type	Best pChEMBL	Mean pChEMBL	Best (nM)	# Data
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform CHEMBL3130	IC50	9.2	8.9167	0.6	3
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform CHEMBL2189158	IC50	9.1	9.1	0.8	1
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta CHEMBL5554	IC50	8.5	8.5	3.2	1
Phosphatidylinositol 3-kinase C2 domain-containing subunit gamma CHEMBL1163120	IC50	7.2	7.2	63.1	1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform CHEMBL4005	IC50	7.2	7.2	63.1	1
Phosphatidylinositol 3-kinase catalytic subunit type 3 CHEMBL1075165	IC50	6.3	6.3	501.2	1
Phosphatidylinositol 4-kinase beta CHEMBL3268	IC50	5.5	5.5	3162.3	1
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha CHEMBL1075102	IC50	5.4	5.4	3981.1	1

Pharmacokinetic Data

Parameter	Value	Units	Species
CL	20.0	mL.min-1.kg-1	Rattus norvegicus
F	4.0	%	Rattus norvegicus
T1/2	2.9	hr	Rattus norvegicus
T1/2	7.1	hr	Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target	Type	Rel.	Value	Units	pChEMBL	Assay	PubMed
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	IC50	=	0.631	nM	9.2	Inhibition of recombinant human PI3Kdelta assessed as reduction in ADP productio...	34080862
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	IC50	=	0.7	nM	9.15	Inhibition of PI3Kdelta (unknown origin)	30582813
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform	IC50	=	0.7943	nM	9.1	Inhibition of PI3Kgamma in C5a-stimulated mouse RAW 264 cells assessed as inhibi...	34080862
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	IC50	=	3.162	nM	8.5	Inhibition of PIK3C2B (unknown origin) assessed as reduction in substrate phosph...	34080862
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	IC50	=	3.981	nM	8.4	Inhibition of PI3Kdelta in anti-IgM-stimulated human JeKo-1 cells assessed as in...	34080862
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform	IC50	=	63.1	nM	7.2	Inhibition of recombinant human PI3Kalpha assessed as reduction in ADP productio...	34080862
Phosphatidylinositol 3-kinase C2 domain-containing subunit gamma	IC50	=	63.1	nM	7.2	Inhibition of PIK3C2G (unknown origin) assessed as reduction in substrate phosph...	34080862
Phosphatidylinositol 3-kinase catalytic subunit type 3	IC50	=	501.19	nM	6.3	Inhibition of PIK3C3 (unknown origin) assessed as reduction in substrate phospho...	34080862
Phosphatidylinositol 4-kinase beta	IC50	=	3162.28	nM	5.5	Inhibition of PI4KB (unknown origin) assessed as reduction in substrate phosphor...	34080862
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha	IC50	=	3981.07	nM	5.4	Inhibition of PIK3C2A (unknown origin) assessed as reduction in substrate phosph...	34080862

Literature References

PubMed	DOI	Target Context	# Activities
34080862	10.1021/acs.jmedchem.1c00434	ADMET	7
30582813	10.1021/acs.jmedchem.8b01298	Unchecked	3
34080862	10.1021/acs.jmedchem.1c00434	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform/gamma isoform	3
34080862	10.1021/acs.jmedchem.1c00434	No relevant target	3
34080862	10.1021/acs.jmedchem.1c00434	Rattus norvegicus	3
34080862	10.1021/acs.jmedchem.1c00434	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	2
35569689	10.1016/j.bmcl.2022.128786	No relevant target	2
30582813	10.1021/acs.jmedchem.8b01298	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	1
34080862	10.1021/acs.jmedchem.1c00434	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform	1
34080862	10.1021/acs.jmedchem.1c00434	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform	1
34080862	10.1021/acs.jmedchem.1c00434	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha	1
34080862	10.1021/acs.jmedchem.1c00434	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	1
34080862	10.1021/acs.jmedchem.1c00434	Phosphatidylinositol 3-kinase C2 domain-containing subunit gamma	1
34080862	10.1021/acs.jmedchem.1c00434	Phosphatidylinositol 3-kinase catalytic subunit type 3	1
34080862	10.1021/acs.jmedchem.1c00434	Phosphatidylinositol 4-kinase alpha	1
34080862	10.1021/acs.jmedchem.1c00434	Phosphatidylinositol 4-kinase beta	1

Data from ChEMBL 36 via Core Engine