General Information of the Protein
Protein ID
PT03697
Protein Name
5-hydroxytryptamine receptor 3A
Secondarily
Protein Name
5-hydroxytryptamine receptor 3
Serotonin receptor 3A
Serotonin-gated ion channel receptor
Gene Name
HTR3A
Secondarily
Gene Name
5ht3
Htr3
Sequence
MRLCIPQVLLALFLSMLTAPGEGSRRRATQARDTTQPALLRLSDHLLANYKKGVRPVRDWRKPTTVSIDVIMYAILNVDEKNQVLTTYIWYRQYWTDEFLQWTPEDFDNVTKLSIPTDSIWVPDILINEFVDVGKSPNIPYVYVHHRGEVQNYKPLQLVTACSLDIYNFPFDVQNCSLTFTSWLHTIQDINITLWRSPEEVRSDKSIFINQGEWELLEVFPQFKEFSIDISNSYAEMKFYVIIRRRPLFYAVSLLLPSIFLMVVDIVGFCLPPDSGERVSFKITLLLGYSVFLIIVSDTLPATAIGTPLIGVYFVVCMALLVISLAETIFIVRLVHKQDLQRPVPDWLRHLVLDRIAWILCLGEQPMAHRPPATFQANKTDDCSGSDLLPAMGNHCSHVGGPQDLEKTPRGRGSPLPPPREASLAVRGLLQELSSIRHFLEKRDEMREVARDWLRVGYVLDRLLFRIYLLAVLAYSITLVTLWSIWHYS
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Organism
Mus musculus, Mouse
Protein Classification
Ion channel
>
Ligand-gated ion channel
>
5HT3 receptor
Function
Forms serotonin (5-hydroxytryptamine/5-HT3)-activated cation-selective channel complexes, which when activated cause fast, depolarizing responses in neurons.
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Uniprot ID
Primary ID:
P23979

Secondarily ID:
E9QLC0
Q61225
Q61226
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Ensembl ID
ENSG00000166736
Subcellular Location
Postsynaptic cell membrane
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: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0056636
10-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-6-fluoro-1,2,10-triazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraen-9-one
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C17H19FN4O
 1
1
EC50 = 178 nM
   TI
   LI
   LO
   TS
CP0056637
10-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-6-chloro-1,2,10-triazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraen-9-one
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C17H19ClN4O
 1
1
EC50 = 178 nM
   TI
   LI
   LO
   TS
CP0120281
10-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-6-methoxy-1,2,10-triazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraen-9-one
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C18H22N4O2
 1
1
EC50 = 178 nM
   TI
   LI
   LO
   TS
CP0120282
10-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-1,2,10-triazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraen-9-one
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C17H20N4O
 1
1
EC50 = 178 nM
   TI
   LI
   LO
   TS
CP0447804
4-(5-Chlorobenzoxazol-2-yl)-1,4-diazabicyclo[3.2.2]nonane
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C14H16ClN3O
 1
1
Ki = 1.2 nM
   TI
   LI
   LO
   TS
CP0376721
4-(5-Methylbenzoxazol-2-yl)-1,4-diazabicyclo[3.2.2]nonane
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C15H19N3O
 1
1
Ki = 3.4 nM
   TI
   LI
   LO
   TS
CP0421782
4-(5-Fluorobenzoxazol-2-yl)-1,4-diazabicyclo[3.2.2]nonane
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C14H16FN3O
 1
1
Ki = 3.9 nM
   TI
   LI
   LO
   TS
CP0197608
4-Benzoxazo-2-yl-1,4-diazabicyclo[3.2.2]nonane
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C14H17N3O
 1
1
Ki = 13 nM
   TI
   LI
   LO
   TS
CP0371836
4-(5-Bromobenzoxazol-2-yl)-1,4-diazabicyclo[3.2.2]nonane
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C14H16BrN3O
 1
1
Ki < 17 nM
   TI
   LI
   LO
   TS
CP0421783
4-(6-Methylbenzoxazol-2-yl)-1,4-diazabicyclo[3.2.2]nonane
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C15H19N3O
 1
1
Ki < 17 nM
   TI
   LI
   LO
   TS
CP0459024
4-Oxazolo[5,4-b]pyridin-2-yl-1,4-diazabicyclo[3.2.2]nonane
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C13H16N4O
 1
1
Ki = 92 nM
   TI
   LI
   LO
   TS
CP0459020
2-(5-Methyloxazolo[5,4-b]pyridin-2-yl)-2,5-diazabicyclo[3.2.2]-nonane
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C14H18N4O
 1
1
Ki = 126 nM
   TI
   LI
   LO
   TS
CP0382768
2-(5-Methoxyoxazolo[4,5-b]pyridin-2-yl)-2,5-diazabicyclo[3.2.2]-nonane
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C14H18N4O2
 1
1
Ki = 141 nM
   TI
   LI
   LO
   TS
CP0382769
4-Oxazolo[5,4-c]pyridin-2-yl-1,4-diazabicyclo[3.2.2]nonane
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C13H16N4O
 1
1
Ki = 162 nM
   TI
   LI
   LO
   TS
CP0080669
4-(6-Chloro-5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo-[3.2.2]nonane
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C14H17ClN4O
 1
1
Ki = 244 nM
   TI
   LI
   LO
   TS
CP0007707
4-(5-Methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]-nonane
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C14H18N4O
 1
1
Ki = 269 nM
   TI
   LI
   LO
   TS
CP0371831
4-(6-Fluoro-5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane
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C14H17FN4O
 1
1
Ki = 547 nM
   TI
   LI
   LO
   TS
CP0191832
4-Oxazolo[4,5-b]pyridin-2-yl-1,4-diazabicyclo[3.2.2]nonane
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C13H16N4O
 1
1
Ki = 579 nM
   TI
   LI
   LO
   TS
CP0060566
4-(6-Bromooxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]-nonane
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C13H15BrN4O
 1
1
Ki = 926 nM
   TI
   LI
   LO
   TS
CP0488652
2-(5-(Piperidin-1-yl)oxazolo[4,5-b]pyridin-2-yl)-2,5-diazabicyclo-[3.2.2]nonane
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C18H25N5O
 1
1
Ki = 1140 nM
   TI
   LI
   LO
   TS
CP0237924
4-(6-Chlorooxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]-nonane
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C13H15ClN4O
 1
1
Ki = 1370 nM
   TI
   LI
   LO
   TS
CP0447806
2-(6-Phenoxyoxazolo[4,5-b]pyridin-2-yl)-2,5-diazabicyclo[3.2.2]-nonane
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C19H20N4O2
 1
1
Ki = 1960 nM
   TI
   LI
   LO
   TS
CP0447805
4-(6-Phenyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]-nonane
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C19H20N4O
 1
1
Ki = 2117 nM
   TI
   LI
   LO
   TS
CP0421784
4-Oxazolo[4,5-c]pyridin-2-yl-1,4-diazabicyclo[3.2.2]nonane
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C13H16N4O
 1
1
Ki = 2120 nM
   TI
   LI
   LO
   TS
CP0481485
4-(6-Methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]-nonane
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C14H18N4O
 1
1
Ki = 3390 nM
   TI
   LI
   LO
   TS
CP0371827
4-(6-Phenyloxazolo[5,4-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]-nonane
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C19H20N4O
 1
1
Ki = 3673 nM
   TI
   LI
   LO
   TS
CP0080659
phenyl 1,4-diazabicyclo[3.2.2]nonane-4-carboxylate
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C14H18N2O2
 1
1
Ki = 3993 nM
   TI
   LI
   LO
   TS
CP0237925
4-(6-Fluorooxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]-nonane
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C13H15FN4O
 1
1
Ki = 6200 nM
   TI
   LI
   LO
   TS
CP0476149
2-(1,4-Diazabicyclo[3.2.2]nonan-4-yl)-5-(pyrrolidin-1-yl)oxazolo-[4,5-b]pyridine
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C17H23N5O
 1
1
Ki = 6340 nM
   TI
   LI
   LO
   TS
CP0371835
2-(5-Phenoxyoxazolo[4,5-b]pyridin-2-yl)-2,5-diazabicyclo[3.2.2]-nonane
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C19H20N4O2
 1
1
Ki = 6830 nM
   TI
   LI
   LO
   TS
CP0371832
2-(5-Phenyloxazolo[4,5-b]pyridin-2-yl)-2,5-diazabicyclo[3.2.2]-nonane
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C19H20N4O
 1
1
Ki > 3580 nM
   TI
   LI
   LO
   TS
CP0034957
2-(5-(2-Fluorophenyl)oxazolo[4,5-b]pyridin-2-yl)-2,5-diazabicyclo[3.2.2]nonane
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C19H19FN4O
 1
1
Ki > 3770 nM
   TI
   LI
   LO
   TS
CP0135869
2-(5-Ethyloxazolo[4,5-b]pyridin-2-yl)-2,5-diazabicyclo[3.2.2]-nonane
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C15H20N4O
 1
1
Ki > 5260 nM
   TI
   LI
   LO
   TS
CP0459021
2-(6-(1H-Pyrazol-3-yl)oxazolo[4,5-b]pyridin-2-yl)-2,5-diazabicyclo[3.2.2]nonane
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C16H18N6O
 1
1
Ki > 5260 nM
   TI
   LI
   LO
   TS
CP0488651
4-(6-Ethyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]-nonane
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C15H20N4O
 1
1
Ki > 5260 nM
   TI
   LI
   LO
   TS
CP0387208
2-(5-Cyclopentyloxazolo[4,5-b]pyridin-2-yl)-2,5-diazabicyclo-[3.2.2]nonane
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C18H24N4O
 1
1
Ki > 5290 nM
   TI
   LI
   LO
   TS
CP0459022
2-(5-Isopropyloxazolo[4,5-b]pyridin-2-yl)-2,5-diazabicyclo[3.2.2]-nonane
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C16H22N4O
 1
1
Ki > 5290 nM
   TI
   LI
   LO
   TS
CP0476148
4-(6-Cyanooxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]-nonane
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C14H15N5O
 1
1
Ki > 5290 nM
   TI
   LI
   LO
   TS
CP0371829
2-(6-(Pyridin-3-yl)oxazolo[4,5-b]pyridin-2-yl)-2,5-diazabicyclo-[3.2.2]nonane
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C18H19N5O
 1
1
Ki > 5350 nM
   TI
   LI
   LO
   TS
CP0371830
2-(6-(Pyrimidine-5-yl)oxazolo[4,5-b]pyridin-2-yl)-2,5-diazabicyclo[3.2.2]nonane
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C17H18N6O
 1
1
Ki > 7140 nM
   TI
   LI
   LO
   TS