AZD-5153

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C25H33N7O3
Molecular Weight	479.5746
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC1=NN=C2C=CC(=NN12)N3CCC(CC3)C4=CC=C(OCCN5CCN(C)C(=O)[C@H]5C)C=C4

InChI

InChIKey=RSMYFSPOTCDHHJ-GOSISDBHSA-N

InChI=1S/C25H33N7O3/c1-18-24(33)29(2)14-15-30(18)16-17-35-21-6-4-19(5-7-21)20-10-12-31(13-11-20)23-9-8-22-26-27-25(34-3)32(22)28-23/h4-9,18,20H,10-17H2,1-3H3/t18-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C25H33N7O3
Molecular Weight	479.5746
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Bromodomain-containing protein 4 13 Target ID: CHEMBL1163125 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27573426	Inhibitor 8504		5.0 nM [IC50]

C_max

Value	Dose	Analyte	Population
34.51 nM CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
21.42 nM CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
62.91 nM CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
245.4 nM CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
232 nM CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
53 nM CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	10 mg 2 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
113.8 nM CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	15 mg 2 times / day multiple, oral dose: 15 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
172.3 nM CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
22.34 nM CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	2 mg 1 times / day multiple, oral dose: 2 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
23.4 nM CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
87.9 nM CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
272.4 nM CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
216 nM CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
48.08 nM CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	10 mg 2 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
106.3 nM CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	15 mg 2 times / day multiple, oral dose: 15 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
109.1 nM CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
83.7 nM × h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
77.82 nM × h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
309.2 nM × h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
604.2 nM × h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
669.2 nM × h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
156.4 nM × h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	10 mg 2 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
272.6 nM × h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	15 mg 2 times / day multiple, oral dose: 15 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
391.1 nM × h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
74.31 nM × h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	2 mg 1 times / day multiple, oral dose: 2 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
102 nM × h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
363.6 nM × h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
650.7 nM × h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
617.6 nM × h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
172.2 nM × h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	10 mg 2 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
316.7 nM × h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	15 mg 2 times / day multiple, oral dose: 15 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
279.2 nM × h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
5.447 h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3.383 h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4.597 h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.643 h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.898 h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.768 h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	10 mg 2 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.164 h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	15 mg 2 times / day multiple, oral dose: 15 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.284 h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
8.753 h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	2 mg 1 times / day multiple, oral dose: 2 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4.88 h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5.193 h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3.727 h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4.15 h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.387 h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	10 mg 2 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.893 h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	15 mg 2 times / day multiple, oral dose: 15 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.33 h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/37486983/	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	AZD-5153 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
23% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27528113/			AZD-5153 plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Substance Class	Chemical Created by `admin` on `Tue Apr 01 21:52:22 GMT 2025` Edited by `admin` on `Tue Apr 01 21:52:22 GMT 2025`
Record UNII	C7C7U6YEAO
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

AZD-5153

Code

English

AZD5153

Preferred Name

English

2-PIPERAZINONE, 4-(2-(4-(1-(3-METHOXY-1,2,4-TRIAZOLO(4,3-B)PYRIDAZIN-6-YL)-4-PIPERIDINYL)PHENOXY)ETHYL)-1,3-DIMETHYL-, (3R)-

Systematic Name

English

AZD 5153 [WHO-DD]

Common Name

English

Code System Code Type Description

PUBCHEM

118693659