Compound Detail

CHEMBL432162

TASOSARTAN

🧪 Phase II

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🧪 Phase II

Cc1nc(C)c2c(n1)N(Cc1ccc(-c3ccccc3-c3nnn[nH]3)cc1)C(=O)CC2

ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID	CHEMBL432162
Name	TASOSARTAN
Phase	Phase II
Structure Type	MOL
InChI Key	ADXGNEYLLLSOAR-UHFFFAOYSA-N

Known Names

ANA-756 Tasosartan WAY-ANA-756

Targets

Activities

Assay Types

PK Parameters

Publications

Known Names

Indications

Mechanisms

Molecular Properties

411.5

MW (Da)

3.42

ALogP

HBA

HBD

100.5

PSA (Å²)

0.55

QED

Ro5 Violations

Rot. Bonds

Drug Information

Molecule Type	Small molecule
Chirality	Achiral

Flags

Natural Product

USAN Stem	-sartan
USAN Year	1995

Extended Properties

Molecular Formula	C23H21N7O
MW	411.47
Aromatic Rings	4
Heavy Atoms	31
NP-Likeness	-1.29

Mechanism of Action

Mechanism	Action Type	Target	Direct	Efficacy
Type-1 angiotensin II receptor antagonist	ANTAGONIST	Type-1 angiotensin II receptor	✓	✓

Indications

Cardiovascular Diseases

ATC Classification

C09CA05

tasosartan

Level 1: CARDIOVASCULAR SYSTEM

Level 2: AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM

Activity Summary

IC50 6 meas. best 8.92

Kd 1 meas. best 8.4

Target Activity Profile

Target	Type	Best pChEMBL	Mean pChEMBL	Best (nM)	# Data
Angiotensin II receptor (AT-1) type-1 CHEMBL2094250	IC50	8.92	8.4933	1.2	3
Angiotensin II receptor CHEMBL2094256	Kd	8.4	8.4	4.0	1
Unchecked CHEMBL612545	IC50	8.28	8.28	5.2	1
Type-1 angiotensin II receptor CHEMBL227	IC50	7.5	7.46	32.0	2

Pharmacokinetic Data

Parameter	Value	Units	Species
AUC	-22669.0	-	-
F	60.0	%	Homo sapiens
T1/2	11.0	hr	-
T1/2	15.0	hr	Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target	Type	Rel.	Value	Units	pChEMBL	Assay	PubMed
Angiotensin II receptor (AT-1) type-1	IC50	=	1.2	nM	8.92	Compound was evaluated for the in vitro inhibition of specific binding of [125I]...	9784100
Angiotensin II receptor	Kd	=	3.981	nM	8.4	Inhibition of angiotensin II-induced contractions in rabbit aorta in vitro.	8576904
Angiotensin II receptor (AT-1) type-1	IC50	=	5.2	nM	8.28	In vitro inhibition of specific binding of [125 I] A II to rat liver membrane.	8120871
Angiotensin II receptor (AT-1) type-1	IC50	=	5.2	nM	8.28	Inhibitory activity against Angiotensin II receptor, type 1 in rat liver membran...	8576904
Unchecked	IC50	=	5.2	nM	8.28	Antagonist activity at angiotensin AT1 receptor in rat liver membranes	21071232
Type-1 angiotensin II receptor	IC50	=	32.0	nM	7.5	Compound was tested for inhibition against Angiotensin II receptor, type 1	12773029
Type-1 angiotensin II receptor	IC50	=	38.0	nM	7.42	Compound was tested in vitro for inhibitory activity against human Angiotensin I...	12113820

Literature References

PubMed	DOI	Target Context	# Activities
15646539	10.1016/s0399-8320(04)95062-2	Unchecked	11
9784100	10.1021/jm970690q	Rattus norvegicus	9
15646539	10.1016/s0399-8320(04)95062-2	NON-PROTEIN TARGET	8
12773029	10.1021/jm0204237	Type-1 angiotensin II receptor	3
15974591	10.1021/jm049024x	Type-1 angiotensin II receptor	3
15974591	10.1021/jm049024x	ADMET	3
22194678	10.1371/journal.pcbi.1002310	Hepatotoxicity	2
8120871	10.1021/jm00030a013	No relevant target	2
12773029	10.1021/jm0204237	ADMET	2
26948801	10.1016/j.drudis.2016.02.015	Homo sapiens	2
37468498	10.1038/s41467-023-40064-9	Thromboxane A2 receptor	2
37468498	10.1038/s41467-023-40064-9	Prostaglandin G/H synthase 1	2
37468498	10.1038/s41467-023-40064-9	D(1A) dopamine receptor	2
8576904	10.1021/jm9504722	Angiotensin II receptor	1
37468498	10.1038/s41467-023-40064-9	Muscarinic acetylcholine receptor M1	1
21071232	10.1016/j.bmc.2010.10.043	Unchecked	1
8576904	10.1021/jm9504722	Rattus norvegicus	1
12113820	10.1016/s0960-894x(02)00303-7	Type-1 angiotensin II receptor	1
9784100	10.1021/jm970690q	Angiotensin II receptor (AT-1) type-1	1
8120871	10.1021/jm00030a013	ADMET	1

Data from ChEMBL 36 via Core Engine