General Information of the Protein
Protein ID
PT02546
Protein Name
Toll-like receptor 8
Gene Name
TLR8
Secondarily
Gene Name
UNQ249/PRO286
Sequence
MENMFLQSSMLTCIFLLISGSCELCAEENFSRSYPCDEKKQNDSVIAECSNRRLQEVPQTVGKYVTELDLSDNFITHITNESFQGLQNLTKINLNHNPNVQHQNGNPGIQSNGLNITDGAFLNLKNLRELLLEDNQLPQIPSGLPESLTELSLIQNNIYNITKEGISRLINLKNLYLAWNCYFNKVCEKTNIEDGVFETLTNLELLSLSFNSLSHVPPKLPSSLRKLFLSNTQIKYISEEDFKGLINLTLLDLSGNCPRCFNAPFPCVPCDGGASINIDRFAFQNLTQLRYLNLSSTSLRKINAAWFKNMPHLKVLDLEFNYLVGEIASGAFLTMLPRLEILDLSFNYIKGSYPQHINISRNFSKLLSLRALHLRGYVFQELREDDFQPLMQLPNLSTINLGINFIKQIDFKLFQNFSNLEIIYLSENRISPLVKDTRQSYANSSSFQRHIRKRRSTDFEFDPHSNFYHFTRPLIKPQCAAYGKALDLSLNSIFFIGPNQFENLPDIACLNLSANSNAQVLSGTEFSAIPHVKYLDLTNNRLDFDNASALTELSDLEVLDLSYNSHYFRIAGVTHHLEFIQNFTNLKVLNLSHNNIYTLTDKYNLESKSLVELVFSGNRLDILWNDDDNRYISIFKGLKNLTRLDLSLNRLKHIPNEAFLNLPASLTELHINDNMLKFFNWTLLQQFPRLELLDLRGNKLLFLTDSLSDFTSSLRTLLLSHNRISHLPSGFLSEVSSLKHLDLSSNLLKTINKSALETKTTTKLSMLELHGNPFECTCDIGDFRRWMDEHLNVKIPRLVDVICASPGDQRGKSIVSLELTTCVSDVTAVILFFFTFFITTMVMLAALAHHLFYWDVWFIYNVCLAKVKGYRSLSTSQTFYDAYISYDTKDASVTDWVINELRYHLEESRDKNVLLCLEERDWDPGLAIIDNLMQSINQSKKTVFVLTKKYAKSWNFKTAFYLALQRLMDENMDVIIFILLEPVLQHSQYLRLRQRICKSSILQWPDNPKAEGLFWQTLRNVVLTENDSRYNNMYVDSIKQY
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Toll-like and Il-1 receptors
Function
Endosomal receptor that plays a key role in innate and adaptive immunity (PubMed:25297876, PubMed:32433612). Controls host immune response against pathogens through recognition of RNA degradation products specific to microorganisms that are initially processed by RNASET2 (PubMed:31778653). Recognizes GU-rich single-stranded RNA (GU-rich RNA) derived from SARS-CoV-2, SARS-CoV-1 and HIV-1 viruses (PubMed:33718825). Upon binding to agonists, undergoes dimerization that brings TIR domains from the two molecules into direct contact, leading to the recruitment of TIR-containing downstream adapter MYD88 through homotypic interaction (PubMed:23520111, PubMed:25599397, PubMed:26929371, PubMed:33718825). In turn, the Myddosome signaling complex is formed involving IRAK4, IRAK1, TRAF6, TRAF3 leading to activation of downstream transcription factors NF-kappa-B and IRF7 to induce pro-inflammatory cytokines and interferons, respectively (PubMed:16737960, PubMed:17932028, PubMed:29155428).
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Uniprot ID
Primary ID:
Q9NR97

Secondarily ID:
B3Y654
D1CS70
D1CS76
Q495P4
Q6UXL6
Q9NYG9
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Ensembl ID
ENSG00000101916
HGNC ID
HGNC:15632
Subcellular Location
Endosome membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000870 , HEK-Blue Null1-v
Compound ID Compound Name Compound Formula
CP0402385
1-(4-amino-2-butyl-7-chloroimidazo[4,5-c]quinolin-1-yl)-2-methylpropan-2-ol
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C18H23ClN4O
 1
1
EC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0473443
1-(4-amino-2-butyl-7-methoxyimidazo[4,5-c]quinolin-1-yl)-2-methylpropan-2-ol
   Show/Hide
C19H26N4O2
 1
1
EC50 = 1700 nM
   TI
   LI
   LO
   TS
CP0233638
1-[4-amino-2-(ethoxymethyl)-1H-imidazo[4,5-c]quinolin-1-yl]-2-methylpropan-2-ol
   Show/Hide
C17H22N4O2
 1
1
EC50 = 3000 nM
   TI
   LI
   LO
   TS
CP0475421
4-amino-2-butyl-1-(2-hydroxy-2-methylpropyl)imidazo[4,5-c]quinoline-7-carbonitrile
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C19H23N5O
 1
1
EC50 = 3900 nM
   TI
   LI
   LO
   TS
CP0541759
1-[4-amino-7-chloro-2-(ethoxymethyl)imidazo[4,5-c]quinolin-1-yl]-2-methylpropan-2-ol
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C17H21ClN4O2
 1
1
EC50 = 4900 nM
   TI
   LI
   LO
   TS
CP0475420
4-amino-2-(ethoxymethyl)-1-(2-hydroxy-2-methylpropyl)imidazo[4,5-c]quinoline-7-carbonitrile
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C18H21N5O2
 1
1
EC50 = 27000 nM
   TI
   LI
   LO
   TS
CP0153455
1-[(4-amino-1-ethyl-7-thiophen-2-ylimidazo[4,5-c]quinolin-2-yl)methyl]pyrrolidin-2-one
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C21H21N5OS
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0153456
(4S)-1-[(4-amino-7-pyrazol-1-yl-3H-imidazo[4,5-c]quinolin-2-yl)methyl]-4-phenylpyrrolidin-2-one
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C24H21N7O
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0153457
N-[(4-amino-7-phenyl-3H-imidazo[4,5-c]quinolin-2-yl)methyl]-N-ethylacetamide
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C21H21N5O
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0179168
N-[[4-amino-1-ethyl-7-(1H-pyrazol-5-yl)imidazo[4,5-c]quinolin-2-yl]methyl]-N-ethylpropanamide
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C21H25N7O
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0188736
N-[[4-amino-7-(cyclopenten-1-yl)-3H-imidazo[4,5-c]quinolin-2-yl]methyl]-N-ethylacetamide
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C20H23N5O
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0188748
tert-butyl N-[[4-amino-1-methyl-7-(1H-pyrazol-5-yl)imidazo[4,5-c]quinolin-2-yl]methyl]-N-ethylcarbamate
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C22H27N7O2
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0238747
2-[[ethyl(methyl)amino]methyl]-7-(1H-pyrazol-5-yl)-3H-imidazo[4,5-c]quinolin-4-amine
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C17H19N7
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0248004
1-[(4-amino-7-phenyl-3H-imidazo[4,5-c]quinolin-2-yl)methyl]pyrrolidin-2-one
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C21H19N5O
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0271059
1-[(4-amino-7-thiophen-2-yl-3H-imidazo[4,5-c]quinolin-2-yl)methyl]pyrrolidin-2-one
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C19H17N5OS
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0271061
1-[[4-amino-7-(3-methylphenyl)-3H-imidazo[4,5-c]quinolin-2-yl]methyl]pyrrolidin-2-one
   Show/Hide
C22H21N5O
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0389374
1-[[4-amino-7-(4-methylphenyl)-3H-imidazo[4,5-c]quinolin-2-yl]methyl]pyrrolidin-2-one
   Show/Hide
C22H21N5O
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0457356
1-[[4-amino-7-(2-fluorophenyl)-3H-imidazo[4,5-c]quinolin-2-yl]methyl]pyrrolidin-2-one
   Show/Hide
C21H18FN5O
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0473444
7-chloro-2-(ethoxymethyl)-1-(2-methylpropyl)imidazo[4,5-c]quinolin-4-amine
   Show/Hide
C17H21ClN4O
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0473445
4-amino-2-butyl-1-(2-methylpropyl)imidazo[4,5-c]quinoline-7-carbonitrile
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C19H23N5
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0475418
4-amino-2-butyl-1-(2-methylpropyl)imidazo[4,5-c]quinolin-7-ol
   Show/Hide
C18H24N4O
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0475422
2-butyl-7-chloro-1-(2-methylpropyl)imidazo[4,5-c]quinolin-4-amine
   Show/Hide
C18H23ClN4
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0520935
4-amino-2-(ethoxymethyl)-1-(2-methylpropyl)imidazo[4,5-c]quinoline-7-carbonitrile
   Show/Hide
C18H21N5O
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0520936
2-butyl-7-methoxy-1-(2-methylpropyl)imidazo[4,5-c]quinolin-4-amine
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C19H26N4O
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0388424
2-[4-[2-(3,4-dimethoxyphenyl)-3-propan-2-yl-1H-indol-5-yl]piperidin-1-yl]-N-methylethanamine
   Show/Hide
C27H37N3O2
 1
1
IC50 = 17 nM
   TI
   LI
   LO
   TS
CP0010966
3-[5-methylsulfanyl-4-(3,4,5-trimethylphenyl)-1,2,4-triazol-3-yl]propan-1-ol
   Show/Hide
C15H21N3OS
 1
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
CP0440907
3-[5-methylsulfanyl-4-(3,4,5-trichlorophenyl)-1,2,4-triazol-3-yl]propan-1-ol
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C12H12Cl3N3OS
 1
1
IC50 = 110 nM
   TI
   LI
   LO
   TS
CP0459341
3-[4-(3,4-dichlorophenyl)-5-methylsulfanyl-1,2,4-triazol-3-yl]propan-1-ol
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C12H13Cl2N3OS
 1
1
IC50 = 190 nM
   TI
   LI
   LO
   TS
CP0574023
3-[5-methylsulfanyl-4-[3-(trifluoromethyl)phenyl]-1,2,4-triazol-3-yl]propan-1-ol
   Show/Hide
C13H14F3N3OS
 1
1
IC50 = 210 nM
   TI
   LI
   LO
   TS
CP0444831
3-[4-(2,4-dichlorophenyl)-5-methylsulfanyl-1,2,4-triazol-3-yl]propan-1-ol
   Show/Hide
C12H13Cl2N3OS
 1
1
IC50 = 290 nM
   TI
   LI
   LO
   TS
CP0558316
3-[4-(3-methylphenyl)-5-methylsulfanyl-1,2,4-triazol-3-yl]propan-1-ol
   Show/Hide
C13H17N3OS
 1
1
IC50 = 290 nM
   TI
   LI
   LO
   TS
CP0440906
3-[4-(3-chlorophenyl)-5-methylsulfanyl-1,2,4-triazol-3-yl]propan-1-ol
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C12H14ClN3OS
 1
1
IC50 = 350 nM
   TI
   LI
   LO
   TS
CP0554769
3-[4-(2,4-dichlorophenyl)-5-ethylsulfanyl-1,2,4-triazol-3-yl]propan-1-ol
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C13H15Cl2N3OS
 1
1
IC50 = 390 nM
   TI
   LI
   LO
   TS
CP0576186
3-(5-methylsulfanyl-4-naphthalen-1-yl-1,2,4-triazol-3-yl)propan-1-ol
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C16H17N3OS
 1
1
IC50 = 390 nM
   TI
   LI
   LO
   TS
CP0554760
5-[4-(2,4-dichlorophenyl)-5-methylsulfanyl-1,2,4-triazol-3-yl]pentan-1-ol
   Show/Hide
C14H17Cl2N3OS
 1
1
IC50 = 520 nM
   TI
   LI
   LO
   TS
CP0548357
[4-(2,4-dichlorophenyl)-5-methylsulfanyl-1,2,4-triazol-3-yl]methanol
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C10H9Cl2N3OS
 1
1
IC50 = 550 nM
   TI
   LI
   LO
   TS
CP0533250
2-[4-(2,4-dichlorophenyl)-5-methylsulfanyl-1,2,4-triazol-3-yl]ethanol
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C11H11Cl2N3OS
 1
1
IC50 = 590 nM
   TI
   LI
   LO
   TS
CP0459342
3-[5-methylsulfanyl-4-(2,3,4-trichlorophenyl)-1,2,4-triazol-3-yl]propan-1-ol
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C12H12Cl3N3OS
 1
1
IC50 = 600 nM
   TI
   LI
   LO
   TS
CP0575213
4-(2,4-dichlorophenyl)-3-methylsulfanyl-5-propyl-1,2,4-triazole
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C12H13Cl2N3S
 1
1
IC50 = 630 nM
   TI
   LI
   LO
   TS
CP0533251
3-[4-(2,3-dichlorophenyl)-5-methylsulfanyl-1,2,4-triazol-3-yl]propan-1-ol
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C12H13Cl2N3OS
 1
1
IC50 = 800 nM
   TI
   LI
   LO
   TS
CP0459340
3-[4-(2-chlorophenyl)-5-methylsulfanyl-1,2,4-triazol-3-yl]propan-1-ol
   Show/Hide
C12H14ClN3OS
 1
1
IC50 = 980 nM
   TI
   LI
   LO
   TS
CP0554759
4-[4-(2,4-dichlorophenyl)-5-methylsulfanyl-1,2,4-triazol-3-yl]butan-1-ol
   Show/Hide
C13H15Cl2N3OS
 1
1
IC50 = 1060 nM
   TI
   LI
   LO
   TS
CP0554761
4-(2,4-dichlorophenyl)-3-(3-methoxypropyl)-5-methylsulfanyl-1,2,4-triazole
   Show/Hide
C13H15Cl2N3OS
 1
1
IC50 = 1180 nM
   TI
   LI
   LO
   TS
CP0548358
3-[4-(4-chlorophenyl)-5-methylsulfanyl-1,2,4-triazol-3-yl]propan-1-ol
   Show/Hide
C12H14ClN3OS
 1
1
IC50 = 1610 nM
   TI
   LI
   LO
   TS
CP0558315
3-[4-(2,4-dichlorophenyl)-5-methylsulfanyl-1,2,4-triazol-3-yl]propyl acetate
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C14H15Cl2N3O2S
 1
1
IC50 = 2080 nM
   TI
   LI
   LO
   TS
CP0539645
3-[5-methylsulfanyl-4-(2,4,6-trichlorophenyl)-1,2,4-triazol-3-yl]propan-1-ol
   Show/Hide
C12H12Cl3N3OS
 1
1
IC50 = 2810 nM
   TI
   LI
   LO
   TS
CP0524989
2-[3-(4-amino-1-benzylimidazo[4,5-c]quinolin-2-yl)propyl]-1-benzylimidazo[4,5-c]quinolin-4-amine
   Show/Hide
C37H32N8
 1
1
IC50 = 3200 nM
   TI
   LI
   LO
   TS
CP0576185
3-[4-(4-methoxyphenyl)-5-methylsulfanyl-1,2,4-triazol-3-yl]propan-1-ol
   Show/Hide
C13H17N3O2S
 1
1
IC50 = 3860 nM
   TI
   LI
   LO
   TS
CP0417283
2-[10-(4-amino-1-benzylimidazo[4,5-c]quinolin-2-yl)decyl]-1-benzylimidazo[4,5-c]quinolin-4-amine
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C44H46N8
 1
1
IC50 = 4650 nM
   TI
   LI
   LO
   TS
CP0385681
N,N'-bis[[4-[(4-amino-2-butylimidazo[4,5-c]quinolin-1-yl)methyl]phenyl]methyl]dodecanediamide
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C56H68N10O2
 1
1
IC50 = 4780 nM
   TI
   LI
   LO
   TS
CP0435788
3-[5-methylsulfanyl-4-[4-(trifluoromethyl)phenyl]-1,2,4-triazol-3-yl]propan-1-ol
   Show/Hide
C13H14F3N3OS
 1
1
IC50 = 4840 nM
   TI
   LI
   LO
   TS
CP0440905
4-(2,4-dichlorophenyl)-3-methylsulfanyl-1H-1,2,4-triazol-5-one
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C9H7Cl2N3OS
 1
1
IC50 = 9000 nM
   TI
   LI
   LO
   TS
CP0459339
3-[4-(2,4-dichlorophenyl)-5-propan-2-ylsulfanyl-1,2,4-triazol-3-yl]propan-1-ol
   Show/Hide
C14H17Cl2N3OS
 1
1
IC50 = 10120 nM
   TI
   LI
   LO
   TS
CP0447821
2-[6-(4-amino-1-benzylimidazo[4,5-c]quinolin-2-yl)hexyl]-1-benzylimidazo[4,5-c]quinolin-4-amine
   Show/Hide
C40H38N8
 1
1
IC50 = 10920 nM
   TI
   LI
   LO
   TS
CP0417282
2-[4-(4-amino-1-benzylimidazo[4,5-c]quinolin-2-yl)butyl]-1-benzylimidazo[4,5-c]quinolin-4-amine
   Show/Hide
C38H34N8
 1
1
IC50 = 15630 nM
   TI
   LI
   LO
   TS
CP0368178
4-(2,4-dichlorophenyl)-3-(3-hydroxypropyl)-1H-1,2,4-triazole-5-thione
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C11H11Cl2N3OS
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0435789
3-(4-cyclohexyl-5-methylsulfanyl-1,2,4-triazol-3-yl)propan-1-ol
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C12H21N3OS
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0444829
S-[[4-(2,4-dichlorophenyl)-5-(3-hydroxypropyl)-1,2,4-triazol-3-yl]] carbamothioate
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C12H12Cl2N4O2S
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0520394
2-[[4-(2,4-dichlorophenyl)-5-(3-hydroxypropyl)-1,2,4-triazol-3-yl]sulfanyl]acetamide
   Show/Hide
C13H14Cl2N4O2S
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0576187
3-(5-methylsulfanyl-4-pyridin-3-yl-1,2,4-triazol-3-yl)propan-1-ol
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C11H14N4OS
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0224537
5-(4-aminobutyl)-4-N-butyl-6-methylpyrimidine-2,4-diamine;dihydrochloride
   Show/Hide
C13H27Cl2N5
 1
1 EC50 = 9260 nM
CP0010966
3-[5-methylsulfanyl-4-(3,4,5-trimethylphenyl)-1,2,4-triazol-3-yl]propan-1-ol
   Show/Hide
C15H21N3OS
 1
1 Kd = 225 nM
Clinical Information about the Protein
Target 1 ( Toll-like receptor 8 (TLR8) )
Target Type Clinical trial Target
Disease 4 Target-related Diseases  4
1 Systemic lupus erythematosus [ICD-11: 4A40.0]
2 Hepatitis B [ICD-11: 1E51]
3 Actinic keratosis [ICD-11: EK90.0]
4 Allergy [ICD-11: 4A80-4A85]
Clinical Trial Drug(s) 3 Clinical Trial Drugs  3
1 Afimetoran Phase 2
Systemic lupus erythematosus
2 Selgantolimod Phase 2
Hepatitis B
3 Resiquimod Phase 2
Actinic keratosis
Discontinued Drug(s) 1 Discontinued Drug  1
1 VTX-2337 Discontinued in Phase 2
Allergy