General Information of the Protein
Protein ID
PT03308
Protein Name
G-protein coupled receptor 35
Secondarily
Protein Name
Kynurenic acid receptor
Gene Name
GPR35
Sequence
MNGTYNTCGSSDLTWPPAIKLGFYAYLGVLLVLGLLLNSLALWVFCCRMQQWTETRIYMTNLAVADLCLLCTLPFVLHSLRDTSDTPLCQLSQGIYLTNRYMSISLVTAIAVDRYVAVRHPLRARGLRSPRQAAAVCAVLWVLVIGSLVARWLLGIQEGGFCFRSTRHNFNSMAFPLLGFYLPLAVVVFCSLKVVTALAQRPPTDVGQAEATRKAARMVWANLLVFVVCFLPLHVGLTVRLAVGWNACALLETIRRALYITSKLSDANCCLDAICYYYMAKEFQEASALAVAPSAKAHKSQDSLCVTLA
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Carboxylic acid receptor
>
Kynurenic acid receptor
Function
G-protein coupled receptor that binds to several ligands including the tryptophan metabolite kynurenic acid (KYNA), lysophosphatidic acid (LPA) or 5-hydroxyindoleacetic acid (5-HIAA) with high affinity, leading to rapid and transient activation of numerous intracellular signaling pathways (PubMed:16754668, PubMed:20361937, PubMed:35148838). Plays a role in neutrophil recruitment to sites of inflammation and bacterial clearance through the major serotonin metabolite 5-HIAA that acts as a physiological ligand (PubMed:35148838). Stimulates lipid metabolism, thermogenic, and anti-inflammatory gene expression in adipose tissue once activated by kynurenic acid (By similarity). In macrophages, activation by lysophosphatidic acid promotes GPR35-induced signaling with a distinct transcriptional profile characterized by TNF production associated with ERK and NF-kappa-B activation. In turn, induces chemotaxis of macrophages (By similarity).
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Uniprot ID
Primary ID:
Q9HC97

Secondarily ID:
J3KR30
O43495
Q17R58
Q4VBN5
Q4ZFV2
Q6FHI8
Q86UH4
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HGNC ID
HGNC:4492
Subcellular Location
Cell 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: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0414285
6-bromo-8-[(3-fluoro-4-methoxybenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C18H11BrFNO6
 2
1
EC50 = 4.37 nM
   TI
   LI
   LO
   TS
2
Ki = 1.64 nM
   TI
   LI
   LO
   TS
CP0389123
6-bromo-8-[(2-fluoro-4-methoxybenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C18H11BrFNO6
 2
1
EC50 = 4.45 nM
   TI
   LI
   LO
   TS
2
Ki = 1.37 nM
   TI
   LI
   LO
   TS
CP0379959
6-bromo-8-[(2,6-difluoro-4-methoxybenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C18H10BrF2NO6
 2
1
EC50 = 5.54 nM
   TI
   LI
   LO
   TS
2
Ki = 0.589 nM
   TI
   LI
   LO
   TS
CP0379961
6-chloro-8-[(2-fluoro-4-methoxybenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C18H11ClFNO6
 2
1
EC50 = 6.06 nM
   TI
   LI
   LO
   TS
2
Ki = 1.92 nM
   TI
   LI
   LO
   TS
CP0395599
6-bromo-8-[(2-chloro-4-methoxybenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C18H11BrClNO6
 3
1
EC50 = 11.1 nM
   TI
   LI
   LO
   TS
2
EC50 = 14.7 nM
   TI
   LI
   LO
   TS
3
Ki = 1.12 nM
   TI
   LI
   LO
   TS
CP0380136
6-bromo-8-[(2,4-dichlorobenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C17H8BrCl2NO5
 3
1
EC50 = 16.4 nM
   TI
   LI
   LO
   TS
2
EC50 = 34.6 nM
   TI
   LI
   LO
   TS
3
Ki = 0.938 nM
   TI
   LI
   LO
   TS
CP0397174
6-chloro-8-[(4-methoxybenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C18H12ClNO6
 3
1
EC50 = 16.8 nM
   TI
   LI
   LO
   TS
2
EC50 = 28.6 nM
   TI
   LI
   LO
   TS
3
Ki = 5.5 nM
   TI
   LI
   LO
   TS
CP0395591
8-[(2,4-dichlorobenzoyl)amino]-6-fluoro-4-oxochromene-2-carboxylic acid
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C17H8Cl2FNO5
 2
1
EC50 = 20.5 nM
   TI
   LI
   LO
   TS
2
Ki = 4.12 nM
   TI
   LI
   LO
   TS
CP0389119
6-bromo-8-[(4-methoxybenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C18H12BrNO6
 2
1
EC50 = 22.1 nM
   TI
   LI
   LO
   TS
2
Ki = 5.18 nM
   TI
   LI
   LO
   TS
CP0395598
6-bromo-8-[(4-chlorobenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C17H9BrClNO5
 3
1
EC50 = 25.1 nM
   TI
   LI
   LO
   TS
2
EC50 = 40.5 nM
   TI
   LI
   LO
   TS
3
Ki = 4.79 nM
   TI
   LI
   LO
   TS
CP0395586
6-bromo-8-[(3,4-dichlorobenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C17H8BrCl2NO5
 3
1
EC50 = 25.1 nM
   TI
   LI
   LO
   TS
2
EC50 = 27.2 nM
   TI
   LI
   LO
   TS
3
Ki = 2.18 nM
   TI
   LI
   LO
   TS
CP0413804
6-methoxy-8-[(4-methoxybenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C19H15NO7
 2
1
EC50 = 25.5 nM
   TI
   LI
   LO
   TS
2
Ki = 20.5 nM
   TI
   LI
   LO
   TS
CP0505056
8-[(4-methoxybenzoyl)amino]-6-methyl-4-oxochromene-2-carboxylic acid
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C19H15NO6
 2
1
EC50 = 37.7 nM
   TI
   LI
   LO
   TS
2
Ki = 42.8 nM
   TI
   LI
   LO
   TS
CP0285587
2-[2-[4-[(4-chlorophenyl)-phenyl-methyl]piperazino]ethoxy]ethanol
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C23H16O6
 3
1
EC50 = 50 nM
   TI
   LI
   LO
   TS
2
EC50 = 1200 nM
   TI
   LI
   LO
   TS
3
Ki = 11.5 nM
   TI
   LI
   LO
   TS
CP0381004
8-(1,3-benzodioxole-5-carbonylamino)-6-bromo-4-oxochromene-2-carboxylic acid
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C18H10BrNO7
 3
1
EC50 = 59.9 nM
   TI
   LI
   LO
   TS
2
EC50 = 128 nM
   TI
   LI
   LO
   TS
3
Ki = 15 nM
   TI
   LI
   LO
   TS
CP0380130
8-[(3,4-dichlorobenzoyl)amino]-6-fluoro-4-oxochromene-2-carboxylic acid
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C17H8Cl2FNO5
 3
1
EC50 = 106 nM
   TI
   LI
   LO
   TS
2
EC50 = 117 nM
   TI
   LI
   LO
   TS
3
Ki = 11.5 nM
   TI
   LI
   LO
   TS
CP0380113
ethyl 6-fluoro-8-[(4-methoxybenzoyl)amino]-4-oxochromene-2-carboxylate
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C20H16FNO6
 2
1
EC50 = 112 nM
   TI
   LI
   LO
   TS
2
Ki = 198 nM
   TI
   LI
   LO
   TS
CP0395601
6-fluoro-8-[(4-methoxybenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C18H12FNO6
 3
1
EC50 = 112 nM
   TI
   LI
   LO
   TS
2
EC50 = 143 nM
   TI
   LI
   LO
   TS
3
Ki = 25.4 nM
   TI
   LI
   LO
   TS
CP0380115
6-bromo-8-[(5-methoxypyridine-2-carbonyl)amino]-4-oxochromene-2-carboxylic acid
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C17H11BrN2O6
 2
1
EC50 = 144 nM
   TI
   LI
   LO
   TS
2
Ki = 56.8 nM
   TI
   LI
   LO
   TS
CP0404055
8-benzamido-6-bromo-4-oxochromene-2-carboxylic acid
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C17H10BrNO5
 2
1
EC50 = 303 nM
   TI
   LI
   LO
   TS
2
Ki = 81.6 nM
   TI
   LI
   LO
   TS
CP0395595
8-[(4-methoxybenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C18H13NO6
 3
1
EC50 = 346 nM
   TI
   LI
   LO
   TS
2
EC50 = 472 nM
   TI
   LI
   LO
   TS
3
Ki = 221 nM
   TI
   LI
   LO
   TS
CP0378851
2-[4-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]acetic acid
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C12H9NO5S
 2
1
EC50 = 349 nM
   TI
   LI
   LO
   TS
2
Ki = 50.8 nM
   TI
   LI
   LO
   TS
CP0395588
8-[(2,3-dichlorobenzoyl)amino]-6-fluoro-4-oxochromene-2-carboxylic acid
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C17H8Cl2FNO5
 3
1
EC50 = 382 nM
   TI
   LI
   LO
   TS
2
EC50 = 873 nM
   TI
   LI
   LO
   TS
3
Ki = 119 nM
   TI
   LI
   LO
   TS
CP0395733
6-bromo-8-[(4-cyanobenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C18H9BrN2O5
 2
1
EC50 = 399 nM
   TI
   LI
   LO
   TS
2
Ki = 148 nM
   TI
   LI
   LO
   TS
CP0389127
8-benzamido-6-chloro-4-oxochromene-2-carboxylic acid
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C17H10ClNO5
 2
1
EC50 = 430 nM
   TI
   LI
   LO
   TS
2
Ki = 138 nM
   TI
   LI
   LO
   TS
CP0389124
6-bromo-8-[(3,4-dimethoxybenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C19H14BrNO7
 2
1
EC50 = 628 nM
   TI
   LI
   LO
   TS
2
Ki = 228 nM
   TI
   LI
   LO
   TS
CP0380116
6-bromo-8-[(4-ethoxybenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C19H14BrNO6
 2
1
EC50 = 634 nM
   TI
   LI
   LO
   TS
2
Ki = 98.4 nM
   TI
   LI
   LO
   TS
CP0378849
8-[(4-bromobenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C17H10BrNO5
 3
1
EC50 = 678 nM
   TI
   LI
   LO
   TS
2
EC50 = 804 nM
   TI
   LI
   LO
   TS
3
Ki = 233 nM
   TI
   LI
   LO
   TS
CP0395590
6-bromo-8-[(3-methylbenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C18H12BrNO5
 3
1
EC50 = 699 nM
   TI
   LI
   LO
   TS
2
EC50 = 842 nM
   TI
   LI
   LO
   TS
3
Ki = 128 nM
   TI
   LI
   LO
   TS
CP0380137
6-chloro-8-[(3-methylbenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C18H12ClNO5
 2
1
EC50 = 1220 nM
   TI
   LI
   LO
   TS
2
Ki = 250 nM
   TI
   LI
   LO
   TS
CP0748604
5-[3-(2-carboxy-4-oxo-4H-5-chromenyloxy)-2-hydroxypropoxy]-4-oxo-4H-2-chromenecarboxylic acid (sodium) (disodium cromoglycate)
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C23H14Na2O11
 1
1
EC50 = 1260 nM
   TI
   LI
   LO
   TS
CP0397194
4-oxo-8-(quinoline-2-carbonylamino)chromene-2-carboxylic acid
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C20H12N2O5
 2
1
EC50 = 1340 nM
   TI
   LI
   LO
   TS
2
Ki = 691 nM
   TI
   LI
   LO
   TS
CP0395602
8-[(4-methylbenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C18H13NO5
 2
1
EC50 = 1380 nM
   TI
   LI
   LO
   TS
2
Ki = 697 nM
   TI
   LI
   LO
   TS
CP0395600
6-chloro-8-[(4-nitrobenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C17H9ClN2O7
 2
1
EC50 = 1710 nM
   TI
   LI
   LO
   TS
2
Ki = 183 nM
   TI
   LI
   LO
   TS
CP0037172
3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0]nona-1,3,6-trien-5-one
   Show/Hide
C13H13N5O2
 3
1
EC50 = 1960 nM
   TI
   LI
   LO
   TS
2
EC50 = 2240 nM
   TI
   LI
   LO
   TS
3
Ki = 401 nM
   TI
   LI
   LO
   TS
CP0395587
8-(cyclohexanecarbonylamino)-4-oxochromene-2-carboxylic acid
   Show/Hide
C17H17NO5
 2
1
EC50 = 4200 nM
   TI
   LI
   LO
   TS
2
Ki = 3580 nM
   TI
   LI
   LO
   TS
CP0381006
8-(naphthalene-2-carbonylamino)-4-oxochromene-2-carboxylic acid
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C21H13NO5
 2
1
EC50 = 4670 nM
   TI
   LI
   LO
   TS
2
Ki = 714 nM
   TI
   LI
   LO
   TS
CP0397173
8-benzamido-4-oxochromene-2-carboxylic acid
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C17H11NO5
 2
1
EC50 = 4910 nM
   TI
   LI
   LO
   TS
2
Ki = 3290 nM
   TI
   LI
   LO
   TS
CP0397175
8-[(3-methylbenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C18H13NO5
 2
1
EC50 = 5440 nM
   TI
   LI
   LO
   TS
2
Ki = 4780 nM
   TI
   LI
   LO
   TS
CP0381000
8-[(3-nitrobenzoyl)amino]-4-oxochromene-2-carboxylic acid
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C17H10N2O7
 2
1
EC50 = 6970 nM
   TI
   LI
   LO
   TS
2
Ki = 4390 nM
   TI
   LI
   LO
   TS
CP0395596
4-oxo-8-[(2-phenylacetyl)amino]chromene-2-carboxylic acid
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C18H13NO5
 2
1
EC50 = 8960 nM
   TI
   LI
   LO
   TS
2
Ki = 2720 nM
   TI
   LI
   LO
   TS
CP0070834
3,3''''-methylenebis(4-hydroxy-coumarin
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C19H12O6
 2
1
EC50 = 9780 nM
   TI
   LI
   LO
   TS
2
Ki = 39 nM
   TI
   LI
   LO
   TS
CP0066118
4-chloro-2-[(furan-2-ylmethyl)amino]-5-sulfamoylbenzoic acid
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C12H11ClN2O5S
 2
1
EC50 = 11200 nM
   TI
   LI
   LO
   TS
2
Ki = 3270 nM
   TI
   LI
   LO
   TS
CP0395597
8-amino-6-bromo-4-oxochromene-2-carboxylic acid
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C10H6BrNO4
 2
1
EC50 = 12600 nM
   TI
   LI
   LO
   TS
2
Ki = 3010 nM
   TI
   LI
   LO
   TS
CP0380135
4-oxo-8-(propanoylamino)chromene-2-carboxylic acid
   Show/Hide
C13H11NO5
 2
1
EC50 = 13400 nM
   TI
   LI
   LO
   TS
2
Ki = 6770 nM
   TI
   LI
   LO
   TS
CP0395589
4-oxo-8-[[4-(trifluoromethyl)benzoyl]amino]chromene-2-carboxylic acid
   Show/Hide
C18H10F3NO5
 2
1
EC50 = 15500 nM
   TI
   LI
   LO
   TS
2
Ki = 10300 nM
   TI
   LI
   LO
   TS
CP0374969
8-[(3-methoxy-3-oxopropanoyl)amino]-4-oxochromene-2-carboxylic acid
   Show/Hide
C14H11NO7
 2
1
EC50 = 20200 nM
   TI
   LI
   LO
   TS
2
Ki = 18600 nM
   TI
   LI
   LO
   TS
CP0378850
8-acetamido-4-oxochromene-2-carboxylic acid
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C12H9NO5
 2
1
EC50 = 24100 nM
   TI
   LI
   LO
   TS
2
Ki = 18500 nM
   TI
   LI
   LO
   TS
CP0084320
CAS_4394-00-7
   Show/Hide
C13H9F3N2O2
 2
1
EC50 = 30800 nM
   TI
   LI
   LO
   TS
2
Ki = 3610 nM
   TI
   LI
   LO
   TS
CP0049039
4-hydroxyquinoline-2-carboxylic acid
   Show/Hide
C10H7NO3
 1
1
EC50 = 39200 nM
   TI
   LI
   LO
   TS
CP0380101
8-nitro-4-oxochromene-2-carboxylic acid
   Show/Hide
C10H5NO6
 2
1
EC50 = 46300 nM
   TI
   LI
   LO
   TS
2
Ki = 13600 nM
   TI
   LI
   LO
   TS
CP0208524
2-hydroxy-4-({4-[5-(2-methyl-3-phenyl-2-propen-1-ylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]butanoyl}amino)benzoic acid
   Show/Hide
C24H22N2O5S2
 2
1
IC50 = 522 nM
   TI
   LI
   LO
   TS
2
Ki = 8.76 nM
   TI
   LI
   LO
   TS
CP0856570
SID99309109
   Show/Hide
C17H19F2N5O2S
 2
1
IC50 = 574 nM
   TI
   LI
   LO
   TS
2
Ki = 42.2 nM
   TI
   LI
   LO
   TS
CP0868920
6-Bromo-8-(4-[3H]methoxybenzamido)-4-oxo-4H-chromene-2-carboxylic acid
   Show/Hide
C18H12BrNO6
 4
1
Kd = 5.27 nM
   TI
   LI
   LO
   TS
2
Kd = 5.65 nM
   TI
   LI
   LO
   TS
3
Kd = 5.92 nM
   TI
   LI
   LO
   TS
4
Kd = 115 nM
   TI
   LI
   LO
   TS
CP0381005
6-bromo-8-[(6-methoxypyridine-3-carbonyl)amino]-4-oxochromene-2-carboxylic acid
   Show/Hide
C17H11BrN2O6
 1
1
Ki = 25.7 nM
   TI
   LI
   LO
   TS
CP0397163
6-bromo-8-[(2-methoxybenzoyl)amino]-4-oxochromene-2-carboxylic acid
   Show/Hide
C18H12BrNO6
 1
1
Ki = 331 nM
   TI
   LI
   LO
   TS
CP0382598
2-[3-cyano-5-(3,4-dichlorophenyl)-4,5-dimethylfuran-2-ylidene]propanedinitrile
   Show/Hide
C16H9Cl2N3O
 1
1
Ki = 655 nM
   TI
   LI
   LO
   TS
CP0082759
CROMOLYN
   Show/Hide
C23H16O11
 1
1
Ki = 2340 nM
   TI
   LI
   LO
   TS
CP0411386
8-[[4-(cyclopropylmethoxy)benzoyl]amino]-4-oxochromene-2-carboxylic acid
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C21H17NO6
 1
1
Ki = 3710 nM
   TI
   LI
   LO
   TS
CP0381003
4-oxo-8-[(4-propoxybenzoyl)amino]chromene-2-carboxylic acid
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C20H17NO6
 1
1
Ki = 8060 nM
   TI
   LI
   LO
   TS
CP0033053
(4S)-2-(6-hydroxy-1,3-benzothiazol-2-yl)-4,5-dihydro-1,3-thiazole-4-carboxylic acid
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C11H8N2O3S2
 1
1
Ki = 9860 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0285587
2-[2-[4-[(4-chlorophenyl)-phenyl-methyl]piperazino]ethoxy]ethanol
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C23H16O6
 1
1 EC50 = 2.1 nM
CP0258522
4-[(Z)-[2-(2-fluorophenyl)imino-4-oxo-1,3-thiazolidin-5-ylidene]methyl]benzoic acid
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C17H11FN2O3S
 1
1 EC50 = 3.2 nM
CP0037172
3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0]nona-1,3,6-trien-5-one
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C13H13N5O2
 1
1 EC50 = 130 nM
CP0082759
CROMOLYN
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C23H16O11
 2
1 EC50 = 210 nM
2 EC50 = 520 nM
CP0084320
CAS_4394-00-7
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C13H9F3N2O2
 1
1 EC50 = 1110 nM
CP0066118
4-chloro-2-[(furan-2-ylmethyl)amino]-5-sulfamoylbenzoic acid
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C12H11ClN2O5S
 1
1 EC50 = 6200 nM
CP0049039
4-hydroxyquinoline-2-carboxylic acid
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C10H7NO3
 1
1 IC50 = 39000 nM
Clinical Information about the Protein
Target 1 ( Kynurenic acid receptor (GPR35) )
Target Type Literature-reported Target