Compound Detail

CHEMBL1231124

AZD-1480

🧪 Phase II

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🧪 Phase II

Cc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)ncc2Cl)[nH]n1

ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID	CHEMBL1231124
Name	AZD-1480
Phase	Phase II
Structure Type	MOL
InChI Key	PDOQBOJDRPLBQU-QMMMGPOBSA-N

Known Names

Azd 1480 Azd-1480 AZD1480

Targets

Activities

Assay Types

PK Parameters

Publications

Known Names

Indications

Mechanisms

Molecular Properties

348.8

MW (Da)

3.01

ALogP

HBA

HBD

104.3

PSA (Å²)

0.65

QED

Ro5 Violations

Rot. Bonds

Drug Information

Molecule Type	Small molecule
Chirality	Single Enantiomer

Extended Properties

Molecular Formula	C14H14ClFN8
MW	348.77
Aromatic Rings	3
Heavy Atoms	24
NP-Likeness	-1.74

Mechanism of Action

Mechanism	Action Type	Target	Direct	Efficacy
Tyrosine-protein kinase JAK2 inhibitor	INHIBITOR	Tyrosine-protein kinase JAK2	✓	✓

Indications

Carcinoma Carcinoma, Hepatocellular Carcinoma, Non-Small-Cell Lung Neoplasms Primary Myelofibrosis Stomach Neoplasms Thrombocythemia, Essential

Activity Summary

IC50 30 meas. best 9.7

Kd 21 meas. best 6.72

Target Activity Profile

Target	Type	Best pChEMBL	Mean pChEMBL	Best (nM)	# Data
Tyrosine-protein kinase JAK1 CHEMBL2835	IC50	9.7	9.4975	0.2	4
Tyrosine-protein kinase JAK2 CHEMBL2971	IC50	9.4	6.7455	0.4	11
Non-receptor tyrosine-protein kinase TYK2 CHEMBL3553	IC50	8.7	8.7	2.0	3
High affinity nerve growth factor receptor CHEMBL2815	IC50	8.52	8.52	3.0	1
Signal transducer and activator of transcription 3 CHEMBL4026	IC50	7.64	7.37	23.0	2
Signal transducer and activator of transcription 5A CHEMBL5403	IC50	7.6	7.495	25.0	2
Unchecked CHEMBL612545	IC50	7.34	7.34	46.0	1
Tyrosine-protein kinase JAK3 CHEMBL2148	IC50	7.22	6.8825	60.0	4
Focal adhesion kinase 1 CHEMBL2695	Kd	6.72	6.72	191.0	1
Proto-oncogene tyrosine-protein kinase receptor Ret CHEMBL2041	Kd	6.62	6.62	238.0	1
Serine/threonine-protein kinase PLK4 CHEMBL3788	Kd	6.51	6.51	308.0	1
Aurora kinase A CHEMBL4722	Kd	6.51	6.51	306.0	1
STE20-related kinase adapter protein alpha CHEMBL1795198	Kd	6.5	6.5	316.0	1
Tyrosine-protein kinase Fer CHEMBL3982	Kd	6.29	6.29	517.0	1
Activated CDC42 kinase 1 CHEMBL4599	Kd	6.29	6.29	515.0	1
STE20-like serine/threonine-protein kinase CHEMBL4202	Kd	6.16	6.16	686.0	1
Serine/threonine-protein kinase STK11 CHEMBL5606	Kd	6.15	6.15	714.0	1
HEL CHEMBL613888	IC50	6.14	6.14	730.0	1
Serine/threonine-protein kinase 10 CHEMBL3981	Kd	6.14	6.14	728.0	1
Fibroblast growth factor receptor 1 CHEMBL3650	Kd	6.11	6.11	777.0	1
Serine/threonine-protein kinase 4 CHEMBL4598	Kd	6.07	6.07	861.0	1
Serine/threonine-protein kinase 3 CHEMBL4708	Kd	6.07	6.07	860.0	1
Cyclin-dependent kinase 3 CHEMBL4442	Kd	6.03	6.03	942.0	1
Non-receptor tyrosine-protein kinase TNK1 CHEMBL5334	Kd	5.9	5.9	1264.0	1
Aurora kinase B CHEMBL2185	Kd	5.81	5.81	1559.0	1
Receptor-type tyrosine-protein kinase FLT3 CHEMBL1974	Kd	5.77	5.77	1685.0	1
Serine/threonine-protein kinase PAK 4 CHEMBL4482	Kd	5.72	5.72	1884.0	1
Protein-tyrosine kinase 2-beta CHEMBL5469	Kd	5.72	5.72	1884.0	1
Casein kinase II subunit alpha' CHEMBL4070	Kd	5.4	5.4	3956.0	1
Unchecked CHEMBL612545	Kd	5.31	5.31	4868.0	1
MDA-MB-468 CHEMBL614335	IC50	5.23	5.23	5870.0	1

Pharmacokinetic Data

Parameter	Value	Units	Species
AUC	20089.15	ng.hr.mL-1	Mus musculus
AUC	122069.5	ng.hr.mL-1	Canis lupus familiaris
CL	0.011	mL.min-1.kg-1	Rattus norvegicus
CL	8.9	mL.min-1.kg-1	Rattus norvegicus
CL	13.5	mL.min-1.kg-1	Mus musculus
CL	2.0	mL.min-1.kg-1	Canis lupus familiaris
F	47.0	%	Rattus norvegicus
F	100.0	%	Mus musculus
F	100.0	%	Canis lupus familiaris
T1/2	4.7	hr	Rattus norvegicus
T1/2	1.5	hr	Mus musculus
T1/2	2.0	hr	Mus musculus
T1/2	6.9	hr	Canis lupus familiaris
T1/2	8.5	hr	Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target	Type	Rel.	Value	Units	pChEMBL	Assay	PubMed
Tyrosine-protein kinase JAK1	IC50	=	0.2	nM	9.7	Biochemical Activity Assay: The assays were performed in 384-well, low volume mi...	-
Tyrosine-protein kinase JAK1	IC50	=	0.2	nM	9.7	Biochemical Activity Assay: The assays were performed in 384-well, low volume mi...	-
Tyrosine-protein kinase JAK1	IC50	=	0.2	nM	9.7	Kinase Assay: A kinase selectivity panel which measures substrate peptide phosph...	-
Tyrosine-protein kinase JAK2	IC50	=	0.4	nM	9.4	Competitive inhibition of JAK2 (unknown origin) in the presence of ATP	32120325
Tyrosine-protein kinase JAK2	IC50	=	0.7	nM	9.15	Kinase Assay: A kinase selectivity panel which measures substrate peptide phosph...	-
Tyrosine-protein kinase JAK2	IC50	=	0.7	nM	9.15	Biochemical Activity Assay: The assays were performed in 384-well, low volume mi...	-
Tyrosine-protein kinase JAK2	IC50	=	0.7	nM	9.15	Biochemical Activity Assay: The assays were performed in 384-well, low volume mi...	-
Tyrosine-protein kinase JAK1	IC50	=	1.3	nM	8.89	Competitive inhibition of JAK1 (unknown origin) in the presence of ATP	32120325
Non-receptor tyrosine-protein kinase TYK2	IC50	=	2.0	nM	8.7	Biochemical Activity Assay: The assays were performed in 384-well, low volume mi...	-
Non-receptor tyrosine-protein kinase TYK2	IC50	=	2.0	nM	8.7	Biochemical Activity Assay: The assays were performed in 384-well, low volume mi...	-
Non-receptor tyrosine-protein kinase TYK2	IC50	=	2.0	nM	8.7	Kinase Assay: A kinase selectivity panel which measures substrate peptide phosph...	-
High affinity nerve growth factor receptor	IC50	=	3.0	nM	8.52	Inhibition of TrkA	21138246
Signal transducer and activator of transcription 3	IC50	=	23.0	nM	7.64	Inhibition of Stat3 phosphorylation in human SET2 cells after 1 hr by Western bl...	21138246
Signal transducer and activator of transcription 5A	IC50	=	25.0	nM	7.6	Inhibition of Stat5 phosphorylation in human SET2 cells after 1 hr by Western bl...	21138246
Signal transducer and activator of transcription 5A	IC50	=	41.0	nM	7.39	Inhibition of Stat5 phosphorylation in human HEL cells after 1 hr by Western blo...	21138246
Unchecked	IC50	=	46.0	nM	7.34	Inhibition of Stat5 phosphorylation in mouse Ba/F3 cells expressing TEL-Jak2	21138246
Tyrosine-protein kinase JAK2	IC50	=	58.0	nM	7.24	Inhibition of JAK2 using 5 mM of ATP	21138246
Tyrosine-protein kinase JAK3	IC50	=	60.0	nM	7.22	Biochemical Activity Assay: The assays were performed in 384-well, low volume mi...	-
Tyrosine-protein kinase JAK3	IC50	=	60.0	nM	7.22	Biochemical Activity Assay: The assays were performed in 384-well, low volume mi...	-
Tyrosine-protein kinase JAK3	IC50	=	60.0	nM	7.22	Kinase Assay: A kinase selectivity panel which measures substrate peptide phosph...	-

Literature References

PubMed	DOI	Target Context	# Activities
21138246	10.1021/jm1011319	Unchecked	15
21138246	10.1021/jm1011319	Mus musculus	12
21138246	10.1021/jm1011319	NON-PROTEIN TARGET	9
26254279	10.18632/oncotarget.4214	Tyrosine-protein kinase JAK2	9
21138246	10.1021/jm1011319	Canis familiaris	6
21138246	10.1021/jm1011319	Signal transducer and activator of transcription 5A	5
-	10.6019/CHEMBL4495565	SARS-CoV-2	4
33691794	10.1186/s13148-021-01037-1	A549	4
21138246	10.1021/jm1011319	Signal transducer and activator of transcription 3	4
21138246	10.1021/jm1011319	Rattus norvegicus	4
29191878	10.1126/science.aan4368	Unchecked	4
-	10.6019/CHEMBL4651402	SARS-CoV-2	2
21138246	10.1021/jm1011319	Tyrosine-protein kinase JAK2	2
-	10.6019/CHEMBL4495564	Replicase polyprotein 1ab	2
21138246	10.1021/jm1011319	No relevant target	2
-	10.6019/CHEMBL4808148	Histone deacetylase 6	2
21138246	10.1021/jm1011319	SW-620	1
29191878	10.1126/science.aan4368	AP2-associated protein kinase 1	1
21138246	10.1021/jm1011319	HEL	1
21138246	10.1021/jm1011319	Liver microsomes	1

Data from ChEMBL 36 via Core Engine