FILGOTINIB

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C21H23N5O3S
Molecular Weight	425.504
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O=C(NC1=NN2C(C=CC=C2C3=CC=C(CN4CCS(=O)(=O)CC4)C=C3)=N1)C5CC5

InChI

InChIKey=RIJLVEAXPNLDTC-UHFFFAOYSA-N

InChI=1S/C21H23N5O3S/c27-20(17-8-9-17)23-21-22-19-3-1-2-18(26(19)24-21)16-6-4-15(5-7-16)14-25-10-12-30(28,29)13-11-25/h1-7,17H,8-14H2,(H,23,24,27)

HIDE SMILES / InChI

Molecular Formula	C21H23N5O3S
Molecular Weight	425.504
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: http://www.glpg.com/filgotinib
Curator's Comment: description was created based on several sources, including: http://adisinsight.springer.com/drugs/800032685 | http://www.glpg.com/docs/view/564327aec62e3-en | http://www.glpg.com/docs/view/5719315eea963-en

Filgotinib (GLPG0634) is a highly selective JAK1 inhibitor. GLPG0634 is a promising drug candidate for the future treatment of autoimmune and inflammatory disorders. It is in phase III clinical trials (initiated mid-2016) for the treatment of rheumatoid arthritis, Crohn's disease and ulcerative colitis. Most common adverse events observed were infections, gastrointestinal disorders and nervous system disorders.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Tyrosine-protein kinase JAK1 36 Target ID: CHEMBL2835 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460\|https://www.ncbi.nlm.nih.gov/pubmed/24417533\|https://www.ncbi.nlm.nih.gov/pubmed/25369270	Inhibitor 8228	10.0 nM [IC50]
Tyrosine-protein kinase JAK1 36 Target ID: CHEMBL2835 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460	Inhibitor 8228	10.0 nM [IC50]
Tyrosine-protein kinase JAK2 53 Target ID: CHEMBL2971 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460	Inhibitor 8228	28.0 nM [IC50]
Tyrosine-protein kinase JAK3 26 Target ID: CHEMBL2148 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460	Inhibitor 8228	810.0 nM [IC50]
Tyrosine-protein kinase TYK2 16 Target ID: CHEMBL3553 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24006460	Inhibitor 8228	116.0 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Crohn's disease 42 Sources: http://adisinsight.springer.com/drugs/800032685 http://www.glpg.com/filgotinib	Primary	Phase III 663	Unknown Approved Use Unknown
Ulcerative colitis 122 Sources: http://adisinsight.springer.com/drugs/800032685 http://www.glpg.com/filgotinib	Primary	Phase III 663	Unknown Approved Use Unknown
Rheumatoid arthritis 313 Sources: http://adisinsight.springer.com/drugs/800032685 https://www.ncbi.nlm.nih.gov/pubmed/25681059 http://www.glpg.com/filgotinib	Primary	Phase III 663	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
2580 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25681059	450 mg 1 times / day multiple, oral dose: 450 mg route of administration: Oral experiment type: MULTIPLE co-administered:	FILGOTINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
4.42 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31797578	450 mg 1 times / day multiple, oral dose: 450 mg route of administration: Oral experiment type: MULTIPLE co-administered:	FILGOTINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1160 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25681059	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	FILGOTINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED

AUC

Value	Dose	Analyte	Population
10200 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25681059	450 mg 1 times / day multiple, oral dose: 450 mg route of administration: Oral experiment type: MULTIPLE co-administered:	FILGOTINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
16.3 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31797578	450 mg 1 times / day multiple, oral dose: 450 mg route of administration: Oral experiment type: MULTIPLE co-administered:	FILGOTINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4844 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25681059	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	FILGOTINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED

T_1/2

Value	Dose	Co-administered	Analyte	Population
7.09 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25681059	450 mg 1 times / day multiple, oral dose: 450 mg route of administration: Oral experiment type: MULTIPLE co-administered:		FILGOTINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
5.68 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25681059	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:		FILGOTINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED

Doses

Dose	Population	Adverse events
450 mg 1 times / day multiple, oral Highest studied dose Dose: 450 mg, 1 times / day Route: oral Route: multiple Dose: 450 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/31797578 Page: p.6	healthy, ADULT n = 47 Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Population Size: 47 Sources: https://pubmed.ncbi.nlm.nih.gov/31797578 Page: p.6	Disc. AE: Skin rash... AEs leading to discontinuation/dose reduction: Skin rash (grade 1, 2.1%) Sources: https://pubmed.ncbi.nlm.nih.gov/31797578 Page: p.6

AEs

AE	Significance	Dose	Population
Skin rash	grade 1, 2.1% Disc. AE	450 mg 1 times / day multiple, oral Highest studied dose Dose: 450 mg, 1 times / day Route: oral Route: multiple Dose: 450 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/31797578 Page: p.6	healthy, ADULT n = 47 Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Population Size: 47 Sources: https://pubmed.ncbi.nlm.nih.gov/31797578 Page: p.6

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 768	inhibitor 1752	inhibitor 1837	inhibitor 1599

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2A6 704 UGT1A1 204 UGT1A4 77 UGT1A6 108 CYP1A2 1509 CYP2B6 799 CYP2E1 876 UGT1A9 116 CYP3A4/5 273 CYP2C8 901 CYP2C19 1463 UGT2B7 146 P-gp 1437 OCT2 638 OCT1 506 OAT3 636 OAT1 595 OATP1B3 700 OCT3 149 BSEP 401 OATP1B1 781 BCRP 691 MATE1 304 OAT2 144 MATE2-K 9	CES1b 4 CES1c 4 CES2 28 P-gp 1527 BCRP 555 OATP1B1 403 OATP1B3 347	CYP1A2 689 CYP2B6 538

Drug as perpetrator

Target	Modality	Activity	Metabolite
OATP1B1 796	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 110 uM]
OCT1 523	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 140 uM]	GS-829845 4
OCT1 523	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 151.6 uM]
OATP1B3 709	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 158 uM]	GS-829845 4
OATP1B3 709	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 168 uM]
OCT3 149	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 188 uM]
OATP1B1 796	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 90 uM]	GS-829845 4
OAT1 599	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >100 uM]
OAT3 638	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >100 uM]
CYP2A6 736	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >105.8 uM]
BSEP 402	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >170 uM]
BCRP 765	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >200 uM]
P-gp 1626	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >200 uM]
CYP1A2 1673	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >224 uM]	GS-829845 4
CYP2A6 736	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >224 uM]	GS-829845 4
CYP2B6 985	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >224 uM]	GS-829845 4
CYP2C19 1537	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >224 uM]	GS-829845 4
CYP2C8 955	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >224 uM]	GS-829845 4
CYP2C9 1803	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >224 uM]	GS-829845 4
CYP2D6 1875	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >224 uM]	GS-829845 4
CYP2E1 964	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >224 uM]	GS-829845 4
CYP3A4/5 330	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >224 uM]	GS-829845 4
MATE1 306	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >300 uM]	GS-829845 4
OAT1 599	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >300 uM]	GS-829845 4
OAT2 146	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >300 uM]
OAT2 146	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >300 uM]	GS-829845 4
OAT3 638	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >300 uM]	GS-829845 4
OCT3 149	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >300 uM]	GS-829845 4
P-gp 1626	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >40 uM]	GS-829845 4
BCRP 765	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >50 uM]	GS-829845 4
BSEP 402	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	no [IC50 >500 uM]	GS-829845 4
UGT1A1 254	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >60 uM]
UGT1A4 80	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >60 uM]
UGT1A6 141	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >60 uM]
UGT1A9 121	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >60 uM]
UGT2B7 157	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >60 uM]
CYP2C19 1537	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >70.6 uM]
CYP2C8 955	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >70.6 uM]
CYP2C9 1803	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >70.6 uM]
CYP2E1 964	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	no [IC50 >70.6 uM]
UGT1A1 254	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >80 uM]	GS-829845 4
UGT1A4 80	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >80 uM]	GS-829845 4
UGT1A6 141	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >80 uM]	GS-829845 4
UGT1A9 121	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >80 uM]	GS-829845 4
UGT2B7 157	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no [IC50 >80 uM]	GS-829845 4
CYP1A2 1673	inducer 1542 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
CYP1A2 1673	inducer 1542 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no	GS-829845 4
CYP2B6 985	inducer 1542 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
CYP2B6 985	inducer 1542 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no	GS-829845 4
CYP3A4 1909	inducer 1542 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
CYP3A4 1909	inducer 1542 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no	GS-829845 4
CYP1A2 1673	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	weak [IC50 >70.6 uM]
CYP2B6 985	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	weak [IC50 >70.6 uM]
CYP2D6 1875	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	weak [IC50 >70.6 uM]
CYP3A4/5 330	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_I100_1.pdf#page=42 Page: 42.0	weak [IC50 >70.6 uM]
MATE2-K 9	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	yes [IC50 10.9 uM]	GS-829845 4
OCT2 639	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	yes [IC50 14.9 uM]	GGS-829845 4
MATE2-K 9	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	yes [IC50 5.21 uM]
MATE1 306	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	yes [IC50 8.63 uM]
OCT2 639	inhibitor 3240 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=17 Page: 17.0	yes [IC50 8.7 uM]

Drug as victim

Target	Modality	Activity
CES2 28	substrate 3326 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=13 Page: 13.0	major
CES1b 4	substrate 3326 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=13 Page: 13.0	minor
CES1c 4	substrate 3326 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=13 Page: 13.0	minor
BCRP 555	substrate 3326 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
OATP1B1 403	substrate 3326 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
OATP1B3 347	substrate 3326 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	no
P-gp 1527	substrate 3326 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=16 Page: 16.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1632	inhibitor 1613 Sources: https://www.pmda.go.jp/drugs/2020/P20201005005/230867000_30200AMX00939_A100_1.pdf#page=9 Page: 9.0

PubMed

Title	Date	PubMed

Patents

Sample Use Guides

In Vivo Use Guide

Daily dose range up to 200 mg

Route of Administration: Oral

In Vitro Use Guide

Filgotinib inhibited IL-2– and IL-4–induced JAK1/JAK3/γc signaling and IFN-αB2–induced JAK1/TYK2 type II receptor signaling most potently. IC50 values ranged from 150 to 760 nM.

Substance Class	Chemical Created by `admin` on `Thu Jul 06 10:42:46 UTC 2023` Edited by `admin` on `Thu Jul 06 10:42:46 UTC 2023`
Record UNII	3XVL385Q0M
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

FILGOTINIB

Official Name

English

GS-6034 FREE BASE

Code

English

CYCLOPROPANECARBOXAMIDE, N-(5-(4-((1,1-DIOXIDO-4-THIOMORPHOLINYL)METHYL)PHENYL)(1,2,4)TRIAZOLO(1,5-A)PYRIDIN-2-YL)-

Systematic Name

English

FILGOTINIB [USAN]

Common Name

English

Filgotinib [WHO-DD]

Common Name

English

filgotinib [INN]

Common Name

English

G-146034

Code

English

G146034

Code

English

N-(5-(4-((1,1-OXO-.LAMBDA.6-THIOMORPHOLIN-4-YL)METHYL)PHENYL((1,2,4)TRIAZOLO(1,5-A)PYRIDIN-2-YL)CYCLOPROPANECARBOXAMIDE

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C129825