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Details

Stereochemistry ABSOLUTE
Molecular Formula C29H37N5O2
Molecular Weight 487.6364
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of GSK-3008348 FREE BASE

SMILES

CC1=NN(C(C)=C1)C2=CC=CC(=C2)[C@@H](CN3CC[C@@H](CCC4=CC=C5CCCN=C5N4)C3)CC(O)=O

InChI

InChIKey=ZMXBIIQMSGOIRZ-RCZVLFRGSA-N
InChI=1S/C29H37N5O2/c1-20-15-21(2)34(32-20)27-7-3-5-24(16-27)25(17-28(35)36)19-33-14-12-22(18-33)8-10-26-11-9-23-6-4-13-30-29(23)31-26/h3,5,7,9,11,15-16,22,25H,4,6,8,10,12-14,17-19H2,1-2H3,(H,30,31)(H,35,36)/t22-,25-/m1/s1

HIDE SMILES / InChI
Molecular Formula C29H37N5O2
Molecular Weight 487.6364
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Approval Year

Unknown
149124
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2849
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
102 pg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
30 μg single, respiratory
dose: 30 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
501 pg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
100 μg single, respiratory
dose: 100 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1922 pg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
300 μg single, respiratory
dose: 300 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
7243 pg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
1000 μg single, respiratory
dose: 1000 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
29393 pg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
3000 μg single, respiratory
dose: 3000 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
285 pg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
30 μg single, respiratory
dose: 30 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1765 pg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
100 μg single, respiratory
dose: 100 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
6850 pg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
300 μg single, respiratory
dose: 300 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
29093 pg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
1000 μg single, respiratory
dose: 1000 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
82205 pg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
3000 μg single, respiratory
dose: 3000 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
10.2 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
100 μg single, respiratory
dose: 100 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
10.1 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
300 μg single, respiratory
dose: 300 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
8.97 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
1000 μg single, respiratory
dose: 1000 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
7.95 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
3000 μg single, respiratory
dose: 3000 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
PubMed

PubMed

TitleDatePubMed
Safety, tolerability and pharmacokinetics of GSK3008348, a novel integrin αvβ6 inhibitor, in healthy participants.
2018 Jun
Substance Class Chemical
Created
by admin
on Wed Apr 02 19:47:31 GMT 2025
Edited
by admin
on Wed Apr 02 19:47:31 GMT 2025
Record UNII
L6EE7H64YF
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
GSK3008348 FREE BASE
Preferred Name English
GSK-3008348 FREE BASE
Common Name English
(?S,3R)-?-[3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenyl]-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]-1-pyrrolidinebutanoic acid
Systematic Name English
1-Pyrrolidinebutanoic acid, ?-[3-(3,5-dimethyl-1H-pyrazol-1-yl)phenyl]-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]-, (?S,3R)-
Systematic Name English
Code System Code Type Description
FDA UNII
L6EE7H64YF
Created by admin on Wed Apr 02 19:47:31 GMT 2025 , Edited by admin on Wed Apr 02 19:47:31 GMT 2025
PRIMARY
PUBCHEM
86272865
Created by admin on Wed Apr 02 19:47:31 GMT 2025 , Edited by admin on Wed Apr 02 19:47:31 GMT 2025
PRIMARY
CAS
1629249-33-7
Created by admin on Wed Apr 02 19:47:31 GMT 2025 , Edited by admin on Wed Apr 02 19:47:31 GMT 2025
PRIMARY
SMS_ID
300000042457
Created by admin on Wed Apr 02 19:47:31 GMT 2025 , Edited by admin on Wed Apr 02 19:47:31 GMT 2025
PRIMARY
Related Record Type Details
HUMAN TRANSFORMING GROWTH FACTOR .BETA.-1
INHIBITION OF ACTIVATION->TARGE
Inhibited Smad2 phosphorylation in a concentration-dependent manner
EC50
Structure of GSK-3008348
SALT/SOLVATE -> PARENT
INTEGRIN ALPHA-V/BETA-6
TARGET->DEGRADER
induced ?v?6 internalization and degradation. ligand-induced ?v?6 integrin internalization following 2?h incubation with NHBE cells.
EC50
Related Record Type Details
Structure of GSK-3008348 FREE BASE
ACTIVE MOIETY
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