Details
Stereochemistry | ACHIRAL |
Molecular Formula | C22H23N5O2 |
Molecular Weight | 389.4503 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1(C)CN(C1)C(=O)C2=CC=C(C=C2)C3=CC=CC4=NC(NC(=O)C5CC5)=NN34
InChI
InChIKey=MPYACSQFXVMWNO-UHFFFAOYSA-N
InChI=1S/C22H23N5O2/c1-22(2)12-26(13-22)20(29)16-10-6-14(7-11-16)17-4-3-5-18-23-21(25-27(17)18)24-19(28)15-8-9-15/h3-7,10-11,15H,8-9,12-13H2,1-2H3,(H,24,25,28)
Molecular Formula | C22H23N5O2 |
Molecular Weight | 389.4503 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Solcitinib (also known as GSK2586184 or GLPG0778) is a selective Janus kinase 1 (JAK1) inhibitor, for the treatment of psoriasis, lupus, and ulcerative colitis. Galapagos NV's collaboration with GlaxoSmithKline has hit a roadblock. It was reported that its Big Pharma partner had hit the brakes on a Phase II study of GSK2586184 for lupus after a first look at the data failed to demonstrate a positive effect. And an exploratory Phase I/II of the same drug for ulcerative colitis was put on hold as investigators review the program.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2835 Sources: https://www.ncbi.nlm.nih.gov/pubmed/?term=25724932 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Palliative | Unknown Approved UseUnknown |
|||
Palliative | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
779.8 ng/mL |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
SOLCITINIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1871.7 ng/mL |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
SOLCITINIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
4787.7 μg × h/L |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
SOLCITINIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
7546.1 μg × h/L |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
SOLCITINIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
7656.32 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/27055521 |
400 mg 2 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
SOLCITINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: FED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
9.7 h |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
SOLCITINIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1.8 h |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
SOLCITINIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 22:00:29 GMT 2025
by
admin
on
Mon Mar 31 22:00:29 GMT 2025
|
Record UNII |
3V7GQ1260K
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Preferred Name | English | ||
|
Systematic Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Code | English | ||
|
Code | English | ||
|
Code | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Code | English | ||
|
Systematic Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
NCI_THESAURUS |
C1967
Created by
admin on Mon Mar 31 22:00:29 GMT 2025 , Edited by admin on Mon Mar 31 22:00:29 GMT 2025
|
||
|
NCI_THESAURUS |
C574
Created by
admin on Mon Mar 31 22:00:29 GMT 2025 , Edited by admin on Mon Mar 31 22:00:29 GMT 2025
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
10047
Created by
admin on Mon Mar 31 22:00:29 GMT 2025 , Edited by admin on Mon Mar 31 22:00:29 GMT 2025
|
PRIMARY | |||
|
C152385
Created by
admin on Mon Mar 31 22:00:29 GMT 2025 , Edited by admin on Mon Mar 31 22:00:29 GMT 2025
|
PRIMARY | |||
|
3V7GQ1260K
Created by
admin on Mon Mar 31 22:00:29 GMT 2025 , Edited by admin on Mon Mar 31 22:00:29 GMT 2025
|
PRIMARY | |||
|
44603362
Created by
admin on Mon Mar 31 22:00:29 GMT 2025 , Edited by admin on Mon Mar 31 22:00:29 GMT 2025
|
PRIMARY | |||
|
100000174858
Created by
admin on Mon Mar 31 22:00:29 GMT 2025 , Edited by admin on Mon Mar 31 22:00:29 GMT 2025
|
PRIMARY | |||
|
1206163-45-2
Created by
admin on Mon Mar 31 22:00:29 GMT 2025 , Edited by admin on Mon Mar 31 22:00:29 GMT 2025
|
PRIMARY | |||
|
CHEMBL3301606
Created by
admin on Mon Mar 31 22:00:29 GMT 2025 , Edited by admin on Mon Mar 31 22:00:29 GMT 2025
|
PRIMARY | |||
|
BC-49
Created by
admin on Mon Mar 31 22:00:29 GMT 2025 , Edited by admin on Mon Mar 31 22:00:29 GMT 2025
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
TARGET -> INHIBITOR |
IC50
|
||
|
TARGETF->WEAK INHIBITOR |
IC50
|
||
|
TARGETF->WEAK INHIBITOR |
IC50
|
||
|
TARGET->WEAK INHIBITOR |
|
||
|
TARGETF->WEAK INHIBITOR |
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
|