General Information of the Protein
Protein ID
PT05068
Protein Name
Glycine receptor subunit alpha-1
Secondarily
Protein Name
Glycine receptor 48 kDa subunit
Glycine receptor strychnine-binding subunit
Gene Name
GLRA1
Sequence
MYSFNTLRLYLWETIVFFSLAASKEAEAARSAPKPMSPSDFLDKLMGRTSGYDARIRPNFKGPPVNVSCNIFINSFGSIAETTMDYRVNIFLRQQWNDPRLAYNEYPDDSLDLDPSMLDSIWKPDLFFANEKGAHFHEITTDNKLLRISRNGNVLYSIRITLTLACPMDLKNFPMDVQTCIMQLESFGYTMNDLIFEWQEQGAVQVADGLTLPQFILKEEKDLRYCTKHYNTGKFTCIEARFHLERQMGYYLIQMYIPSLLIVILSWISFWINMDAAPARVGLGITTVLTMTTQSSGSRASLPKVSYVKAIDIWMAVCLLFVFSALLEYAAVNFVSRQHKELLRFRRKRRHHKSPMLNLFQEDEAGEGRFNFSAYGMGPACLQAKDGISVKGANNSNTTNPPPAPSKSPEEMRKLFIQRAKKIDKISRIGFPMAFLIFNMFYWIIYKIVRREDVHNQ
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Organism
Homo sapiens, Human
Protein Classification
Ion channel
>
Ligand-gated ion channel
>
Glycine receptor
Function
Glycine receptors are ligand-gated chloride channels (PubMed:23994010, PubMed:25730860). Channel opening is triggered by extracellular glycine (PubMed:2155780, PubMed:7920629, PubMed:14551753, PubMed:16144831, PubMed:22715885, PubMed:22973015, PubMed:25973519, PubMed:9009272). Channel opening is also triggered by taurine and beta-alanine (PubMed:16144831, PubMed:9009272). Channel characteristics depend on the subunit composition; heteropentameric channels are activated by lower glycine levels and display faster desensitization (PubMed:14551753). Plays an important role in the down-regulation of neuronal excitability (PubMed:8298642, PubMed:9009272). Contributes to the generation of inhibitory postsynaptic currents (PubMed:25445488). Channel activity is potentiated by ethanol (PubMed:25973519). Potentiation of channel activity by intoxicating levels of ethanol contribute to the sedative effects of ethanol (By similarity).
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Uniprot ID
Primary ID:
P23415

Secondarily ID:
B2R6T3
Q14C77
Q6DJV9
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HGNC ID
HGNC:4326
Subcellular Location
Postsynaptic cell membrane
Synapse
Perikaryon
Cell projection
Dendrite
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
CP0853022
8-hydroxyircinialactam B
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C27H39NO7
 1
1
EC50 = 500 nM
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CP0914087
(12E,20Z,18S)-8-hydroxy-variabilin
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C25H36O5
 1
1
EC50 = 1200 nM
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CP0008055
(4aR,5aS,8aR,13aS,15E,15aR,15bR)-15-prop-2-enoxyimino-2,4a,5,5a,7,8,13a,15a,15b,16-decahydro4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-14-one
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C24H25N3O3
 2
1
IC50 = 49 nM
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2
Ki = 370 nM
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CP0003097
CHEBI:28973
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C21H22N2O2
 3
1
IC50 = 50 nM
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2
IC50 = 51 nM
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3
Ki = 23 nM
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CP0009017
(4aR,5aS,8aR,13aS,15E,15aR,15bR)-15-prop-2-ynoxyimino-2,4a,5,5a,7,8,13a,15a,15b,16-decahydro4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-14-one
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C24H23N3O3
 1
1
IC50 = 59 nM
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CP0008081
(4aR,5aS,8aR,13aS,15E,15aR,15bR)-15-methoxyimino-2,4a,5,5a,7,8,13a,15a,15b,16-decahydro4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-14-one
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C22H23N3O3
 2
1
IC50 = 75 nM
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2
Ki = 189 nM
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CP0003095
(4aR,5aS,8aR,13aS,15aS,15bR)-10-amino-4a,5,5a,7,8,13a,15,15a,15b,16-decahydro-2H-4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-14-one
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C21H23N3O2
 1
1
IC50 = 76 nM
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CP0010498
(4aR,5aS,8aR,13aS,15E,15aR,15bR)-15-hydroxyimino-2,4a,5,5a,7,8,13a,15a,15b,16-decahydro4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-14-one
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C21H21N3O3
 2
1
IC50 = 82 nM
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2
Ki = 40 nM
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CP0008292
N-[2-[[(4aR,5aS,8aR,13aS,15aS,15bR)-14-oxo-4a,5,5a,7,8,13a,15,15a,15b,16-decahydro-2H-4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-10-yl]amino]-2-oxoethyl]octanamide
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C31H40N4O4
 1
1
IC50 = 90 nM
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CP0014664
N,N'-bis[2-[[(4aR,5aS,8aR,13aS,15aS,15bR)-14-oxo-4a,5,5a,7,8,13a,15,15a,15b,16-decahydro-2H-4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-10-yl]amino]-2-oxoethyl]dodecanediamide
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C58H70N8O8
 1
1
IC50 = 100 nM
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CP0008849
(4aR,5aS,8aR,13aS,15E,15aR,15bR)-15-propoxyimino-2,4a,5,5a,7,8,13a,15a,15b,16-decahydro4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-14-one
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C24H27N3O3
 2
1
IC50 = 109 nM
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2
Ki = 241 nM
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CP0014662
N,N'-bis[2-[[(4aR,5aS,8aR,13aS,15aS,15bR)-14-oxo-4a,5,5a,7,8,13a,15,15a,15b,16-decahydro-2H-4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-10-yl]amino]-2-oxoethyl]heptanediamide
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C53H60N8O8
 1
1
IC50 = 130 nM
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CP0014663
N,N'-bis[2-[[(4aR,5aS,8aR,13aS,15aS,15bR)-14-oxo-4a,5,5a,7,8,13a,15,15a,15b,16-decahydro-2H-4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-10-yl]amino]-2-oxoethyl]octanediamide
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C54H62N8O8
 1
1
IC50 = 170 nM
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CP0011374
N-[(4aR,5aS,8aR,13aS,15aS,15bR)-14-oxo-4a,5,5a,7,8,13a,15,15a,15b,16-decahydro-2H-4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-10-yl]propanamide
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C24H27N3O3
 2
1
IC50 = 201 nM
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2
Ki = 67 nM
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CP0010011
N,N'-bis[2-[[(4aR,5aS,8aR,13aS,15aS,15bR)-14-oxo-4a,5,5a,7,8,13a,15,15a,15b,16-decahydro-2H-4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-10-yl]amino]-2-oxoethyl]nonanediamide
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C55H64N8O8
 1
1
IC50 = 400 nM
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CP0871088
ginkgolide M
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C20H24O10
 1
1
IC50 = 650 nM
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CP0013664
N,N'-bis[(4aR,5aS,8aR,13aS,15aS,15bR)-14-oxo-4a,5,5a,7,8,13a,15,15a,15b,16-decahydro-2H-4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-10-yl]dodecanediamide
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C54H64N6O6
 1
1
IC50 = 720 nM
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CP0008291
N,N'-bis[(4aR,5aS,8aR,13aS,15aS,15bR)-14-oxo-4a,5,5a,7,8,13a,15,15a,15b,16-decahydro-2H-4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-10-yl]octanediamide
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C50H56N6O6
 1
1
IC50 = 1100 nM
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CP0010012
N,N'-bis[11-[[(4aR,5aS,8aR,13aS,15aS,15bR)-14-oxo-4a,5,5a,7,8,13a,15,15a,15b,16-decahydro-2H-4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-10-yl]amino]-11-oxoundecyl]octanediamide
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C72H98N8O8
 1
1
IC50 = 1400 nM
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CP0011897
N,N'-bis[(4aR,5aS,8aR,13aS,15aS,15bR)-14-oxo-4a,5,5a,7,8,13a,15,15a,15b,16-decahydro-2H-4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-10-yl]decanediamide
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C52H60N6O6
 1
1
IC50 = 1500 nM
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CP0180510
BN 52021
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C20H24O10
 1
1
IC50 = 1700 nM
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CP0373504
(1R,3R,6R,7S,8S,9S,11S,12S,13S,16S,17S)-8-tert-butyl-6,9,12,17-tetrahydroxy-13-methyl-2,4,15,19-tetraoxahexacyclo[8.7.2.01,11.03,7.07,11.012,16]nonadecane-5,14,18-trione
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C20H24O11
 2
1
IC50 = 1700 nM
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2
IC50 = 5900 nM
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CP0007993
N-[(4aR,5aS,8aR,13aS,15aS,15bR)-14-oxo-4a,5,5a,7,8,13a,15,15a,15b,16-decahydro-2H-4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-10-yl]-11-(octanoylamino)undecanamide
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C40H58N4O4
 1
1
IC50 = 1700 nM
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CP0014665
N,N'-bis[11-[[(4aR,5aS,8aR,13aS,15aS,15bR)-14-oxo-4a,5,5a,7,8,13a,15,15a,15b,16-decahydro-2H-4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-10-yl]amino]-11-oxoundecyl]docosanediamide
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C86H126N8O8
 1
1
IC50 = 2900 nM
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CP0011899
N,N'-bis[11-[[(4aR,5aS,8aR,13aS,15aS,15bR)-14-oxo-4a,5,5a,7,8,13a,15,15a,15b,16-decahydro-2H-4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-10-yl]amino]-11-oxoundecyl]dodecanediamide
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C76H106N8O8
 1
1
IC50 = 3100 nM
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CP0048517
(1R,3R,6R,7S,8S,10R,11S,13S,16S,17R)-8-tert-butyl-6,17-dihydroxy-16-methyl-2,4,14,19-tetraoxahexacyclo[8.7.2.01,11.03,7.07,11.013,17]nonadecane-5,15,18-trione
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C20H24O9
 1
1
IC50 = 3800 nM
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CP0003098
(4aR,5aS,8aS,13aS,15aS,15bR)-6-propyl-4a,5,5a,7,8,13a,15,15a,15b,16-decahydro-2H-4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-6-ium-14-one;bromide
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C24H29BrN2O2
 1
1
IC50 = 4590 nM
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CP0425003
(1S,3R,6R,7S,8S,9S,11S,12S,13S,16S)-8-tert-butyl-6,9,12-trihydroxy-13-methyl-2,4,15,19-tetraoxahexacyclo[8.7.2.01,11.03,7.07,11.012,16]nonadecane-5,14,18-trione
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C20H24O10
 1
1
IC50 = 6400 nM
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CP0373509
(1S,6R,8S,11S,13R,16R,17R)-8-tert-butyl-6,17-dihydroxy-16-methyl-2,4,14,19-tetraoxahexacyclo[8.7.2.0^{1,11}.0^{3,7}.0^{7,11}.0^{13,17}]nonadecane-5,18-dione
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C20H26O8
 1
1
IC50 > 100000 nM
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CP0405700
[(1R,6R,8S,11S,13S,16R,17S)-8-tert-butyl-16-methyl-5,15,18-trioxo-2,4,14,19-tetraoxahexacyclo[8.7.2.01,11.03,7.07,11.013,17]nonadecan-6-yl] acetate
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C22H26O9
 1
1
IC50 > 100000 nM
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CP0441951
(1S,6R,8S,9S,11R,12R,13S,16S,17R)-8-tert-butyl-6,12,17-trihydroxy-16-methyl-5,15,18-trioxo-2,4,14,19-tetraoxahexacyclo[8.7.2.0^{1,11}.0^{3,7}.0^{7,11}.0^{13,17}]nonadecan-9-yl acetate
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C22H26O12
 1
1
IC50 > 100000 nM
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CP0441952
(1S,6R,8S,9S,11R,12R,13S,16S,17R)-8-tert-butyl-9-(ethylamino)-6,12,17-trihydroxy-16-methyl-2,4,14,19-tetraoxahexacyclo[8.7.2.0^{1,11}.0^{3,7}.0^{7,11}.0^{13,17}]nonadecane-5,15,18-trione
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C22H29NO10
 1
1
IC50 > 100000 nM
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CP0441953
(1R,2R,3S,6S,8S,10R,11R)-10-tert-butyl-2,11,16-trihydroxy-3-methyl-5,13,15-trioxapentacyclo[7.5.2.0^{1,8}.0^{2,6}.0^{8,12}]hexadecane-4,14-dione
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C18H24O8
 1
1
IC50 > 100000 nM
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CP0441958
(1S,6R,8S,11R,12R,13S,16S,17R)-8-tert-butyl-6,12,17-trihydroxy-16-methyl-2,4,14,19-tetraoxahexacyclo[8.7.2.0^{1,11}.0^{3,7}.0^{7,11}.0^{13,17}]nonadecane-5,9,15,18-tetrone
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C20H22O11
 1
1
IC50 > 100000 nM
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CP0445825
1,2;3,14-dianhydro-ginkgolide C
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C20H20O9
 1
1
IC50 > 100000 nM
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CP0445836
(1S,6R,8S,9S,11R,12R,13S,16S,17R)-8-tert-butyl-6,12,17-trihydroxy-16-methyl-5,15,18-trioxo-2,4,14,19-tetraoxahexacyclo[8.7.2.0^{1,11}.0^{3,7}.0^{7,11}.0^{13,17}]nonadecan-9-yl 2-phenylacetate
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C28H30O12
 1
1
IC50 > 100000 nM
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CP0486277
(1S,6R,8S,9S,11R,12R,13S,16S,17R)-8-tert-butyl-6,9,12,17-tetrahydroxy-16-methyl-2,4,14,19-tetraoxahexacyclo[8.7.2.0^{1,11}.0^{3,7}.0^{7,11}.0^{13,17}]nonadecane-5,15,18-trione
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C20H24O11
 1
1
IC50 > 100000 nM
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CP0498087
(1S,6R,8S,11S,13S,16R,17R)-8-tert-butyl-6,17-dihydroxy-16-methyl-2,4,14,19-tetraoxahexacyclo[8.7.2.0^{1,11}.0^{3,7}.0^{7,11}.0^{13,17}]nonadecan-18-one
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C20H28O7
 1
1
IC50 > 100000 nM
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CP0502368
methyl (2E)-2-[(1R,6R,8S,11S)-8-tert-butyl-6-hydroxy-5,15-dioxo-2,4,16-trioxapentacyclo[8.4.2.01,11.03,7.07,11]hexadecan-14-ylidene]propanoate
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C21H26O8
 1
1
IC50 > 100000 nM
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CP0373510
methyl 2-[(1R,6R,8S,11S,14R)-8-tert-butyl-6-hydroxy-5,15-dioxo-2,4,16-trioxapentacyclo[8.4.2.01,11.03,7.07,11]hexadecan-14-yl]propanoate
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C21H28O8
 1
1
IC50 > 100000 nM
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CP0435621
(1S,6R,8S,9R,11S,12R,13S,16S,17R)-8-tert-butyl-6,12,17-trihydroxy-16-methyl-5,15,18-trioxo-2,4,14,19-tetraoxahexacyclo[8.7.2.0^{1,11}.0^{3,7}.0^{7,11}.0^{13,17}]nonadecan-9-yl trifluoromethanesulfonate
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C21H23F3O13S
 1
1
IC50 > 100000 nM
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CP0435622
(1S,6R,8S,9S,11R,12R,13S,16S,17R)-8-tert-butyl-6,12,17-trihydroxy-16-methyl-9-(methylamino)-2,4,14,19-tetraoxahexacyclo[8.7.2.0^{1,11}.0^{3,7}.0^{7,11}.0^{13,17}]nonadecane-5,15,18-trione
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C21H27NO10
 1
1
IC50 > 100000 nM
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CP0435625
(1S,8S,11S,13S,16S,17R)-8-tert-butyl-17-hydroxy-16-methyl-2,4,14,19-tetraoxahexacyclo[8.7.2.0^{1,11}.0^{3,7}.0^{7,11}.0^{13,17}]nonadecane-5,6,15,18-tetrone
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C20H22O9
 1
1
IC50 > 100000 nM
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CP0441954
(1R,6R,8S,11S)-8-tert-butyl-6,13-dimethoxy-2,4,14,17-tetraoxapentacyclo[8.5.2.0^{1,11}.0^{3,7}.0^{7,11}]heptadecane-5,15,16-trione
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C19H24O9
 1
1
IC50 > 100000 nM
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CP0441956
10-methoxymethyloxy-ginkgolide A
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C22H28O10
 1
1
IC50 > 100000 nM
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CP0445829
(1R,6R,8S,11S,13S,16R,17R)-8-tert-butyl-16-methyl-2,4,14,19-tetraoxahexacyclo[8.7.2.0^{1,11}.0^{3,7}.0^{7,11}.0^{13,17}]nonadecane-6,17-diol
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C20H30O6
 1
1
IC50 > 100000 nM
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CP0445831
(1R,6R,8S,11R)-8-tert-butyl-13-methoxy-5,15,16-trioxo-2,4,14,17-tetraoxapentacyclo[8.5.2.0^{1,11}.0^{3,7}.0^{7,11}]heptadecan-6-yl acetate
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C20H24O10
 1
1
IC50 > 100000 nM
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CP0445833
(1S,2R,3S,6S,8S,10R)-10-tert-butyl-2-hydroxy-3-methyl-5,13,15-trioxapentacyclo[7.5.2.0^{1,8}.0^{2,6}.0^{8,12}]hexadecane-4,14,16-trione
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C18H22O7
 1
1
IC50 > 100000 nM
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CP0486272
(6R,8S,11S,16R,17S)-8-tert-butyl-6,16,17-trihydroxy-16-methyl-2,4,14,19-tetraoxahexacyclo[8.7.2.0^{1,11}.0^{3,7}.0^{7,11}.0^{13,17}]nonadecane-5,15,18-trione
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C20H24O10
 1
1
IC50 > 100000 nM
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CP0498088
methyl (2R)-2-[(1S,2R,3S,6S,8S,10S)-10-tert-butyl-2-hydroxy-16-methoxy-3-methyl-4,14-dioxo-5,13,15-trioxapentacyclo[7.5.2.01,8.02,6.08,12]hexadecan-9-yl]-2-methoxyacetate
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C23H32O10
 1
1
IC50 > 100000 nM
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CP0505243
10-acetoxy-ginkgolide B
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C22H26O10
 1
1
IC50 > 100000 nM
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CP0000589
Alcuronium
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C44H50N4O2+2
 1
1
IC50 > 100000 nM
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CP0001237
(1R,9R,18S,19S,21R,22R,23R,25R,32S,34R,35R,36S)-24-phenyl-10,26-dioxa-8,15,24,31-tetraazaundecacyclo[29.5.2.0^{1,32}.0^{2,7}.0^{8,36}.0^{9,22}.0^{13,21}.0^{15,19}.0^{18,23}.0^{25,35}.0^{29,34}]octatriaconta-2,4,6,12,28-pentaene
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C38H42N4O2
 1
1
IC50 > 100000 nM
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CP0633393
[(20-{[dimethyl(prop-2-en-1-yl)azaniumyl]methyl}-3,13-diazapentacyclo[11.7.0.0^{3,11}.0^{4,9}.0^{14,19}]icosa-1(20),4,6,8,10,14(19),15,17-octaen-10-yl)methyl]dimethylprop-2-en-1-ylazanium dibromide
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C30H38Br2N4
 1
1
IC50 > 100000 nM
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CP0633394
(1S,11S,13S,17R,18R,20R,27S,29R,30R,31S,35E)-35-(2-hydroxyethylidene)-14,26-dimethyl-19-phenyl-21-oxa-8,14,19,26-tetraazadecacyclo[24.5.2.2^{11,14}.0^{1,27}.0^{2,7}.0^{8,31}.0^{10,18}.0^{13,17}.0^{20,30}.0^{24,29}]pentatriaconta-2,4,6,9,23-pentaene-14,26-diium diiodide
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C40H48I2N4O2
 1
1
IC50 > 100000 nM
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CP0633395
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-dibenzyl-24-phenyl-10,26-dioxa-8,15,24,31-tetraazaundecacyclo[29.5.2.0^{1,32}.0^{2,7}.0^{8,36}.0^{9,22}.0^{13,21}.0^{15,19}.0^{18,23}.0^{25,35}.0^{29,34}]octatriaconta-2,4,6,12,28-pentaene-15,31-diium dibromide
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C52H56Br2N4O2
 1
1
IC50 > 100000 nM
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CP0633396
(1R,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-24-phenyl-15-(prop-2-en-1-yl)-10,26-dioxa-8,15,24,31-tetraazaundecacyclo[29.5.2.0^{1,32}.0^{2,7}.0^{8,36}.0^{9,22}.0^{13,21}.0^{15,19}.0^{18,23}.0^{25,35}.0^{29,34}]octatriaconta-2,4,6,12,28-pentaen-15-ium bromide
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C41H47BrN4O2
 1
1
IC50 > 100000 nM
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CP0633629
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-bis[(3,4-dimethoxyphenyl)methyl]-24-phenyl-10,26-dioxa-8,15,24,31-tetraazaundecacyclo[29.5.2.0^{1,32}.0^{2,7}.0^{8,36}.0^{9,22}.0^{13,21}.0^{15,19}.0^{18,23}.0^{25,35}.0^{29,34}]octatriaconta-2,4,6,12,28-pentaene-15,31-diium dichloride
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C56H64Cl2N4O6
 1
1
IC50 > 100000 nM
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CP0633630
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-bis(cyclohex-2-en-1-yl)-24-phenyl-10,26-dioxa-8,15,24,31-tetraazaundecacyclo[29.5.2.0^{1,32}.0^{2,7}.0^{8,36}.0^{9,22}.0^{13,21}.0^{15,19}.0^{18,23}.0^{25,35}.0^{29,34}]octatriaconta-2,4,6,12,28-pentaene-15,31-bis(ylium) dibromide
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C50H60Br2N4O2
 1
1
IC50 > 100000 nM
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CP0633631
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-24-phenyl-15,31-bis(prop-2-en-1-yl)-10,26-dioxa-8,15,24,31-tetraazaundecacyclo[29.5.2.0^{1,32}.0^{2,7}.0^{8,36}.0^{9,22}.0^{13,21}.0^{15,19}.0^{18,23}.0^{25,35}.0^{29,34}]octatriaconta-2,4,6,12,28-pentaene-15,31-diium dibromide
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C44H52Br2N4O2
 1
1
IC50 > 100000 nM
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CP0633632
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-bis[(4-bromophenyl)methyl]-24-phenyl-10,26-dioxa-8,15,24,31-tetraazaundecacyclo[29.5.2.0^{1,32}.0^{2,7}.0^{8,36}.0^{9,22}.0^{13,21}.0^{15,19}.0^{18,23}.0^{25,35}.0^{29,34}]octatriaconta-2,4,6,12,28-pentaene-15,31-diium dibromide
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C52H54Br4N4O2
 1
1
IC50 > 100000 nM
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CP0633633
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-bis[(4-nitrophenyl)methyl]-24-phenyl-10,26-dioxa-8,15,24,31-tetraazaundecacyclo[29.5.2.0^{1,32}.0^{2,7}.0^{8,36}.0^{9,22}.0^{13,21}.0^{15,19}.0^{18,23}.0^{25,35}.0^{29,34}]octatriaconta-2,4,6,12,28-pentaene-15,31-diium dibromide
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C52H54Br2N6O6
 1
1
IC50 > 100000 nM
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CP0633634
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-bis[2-(acetyloxy)ethyl]-24-phenyl-10,26-dioxa-8,15,24,31-tetraazaundecacyclo[29.5.2.0^{1,32}.0^{2,7}.0^{8,36}.0^{9,22}.0^{13,21}.0^{15,19}.0^{18,23}.0^{25,35}.0^{29,34}]octatriaconta-2,4,6,12,28-pentaene-15,31-diium dibromide
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C46H56Br2N4O6
 1
1
IC50 > 100000 nM
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CP0633635
toxiferine
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C40H46Cl2N4O2
 1
1
IC50 > 100000 nM
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CP0633846
{[20-({dimethyl[(4-nitrophenyl)methyl]azaniumyl}methyl)-3,13-diazapentacyclo[11.7.0.0^{3,11}.0^{4,9}.0^{14,19}]icosa-1(20),4,6,8,10,14(19),15,17-octaen-10-yl]methyl}dimethyl[(4-nitrophenyl)methyl]azanium dibromide
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C38H40Br2N6O4
 1
1
IC50 > 100000 nM
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CP0633847
(1S,11S,13S,17R,18R,20R,27S,29R,30R,31S,35E)-14,26-bis[(3,4-dimethoxyphenyl)methyl]-35-(2-hydroxyethylidene)-19-phenyl-21-oxa-8,14,19,26-tetraazadecacyclo[24.5.2.2^{11,14}.0^{1,27}.0^{2,7}.0^{8,31}.0^{10,18}.0^{13,17}.0^{20,30}.0^{24,29}]pentatriaconta-2,4,6,9,23-pentaene-14,26-diium dichloride
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C56H64Cl2N4O6
 1
1
IC50 > 100000 nM
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CP0633848
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-bis[(2E)-but-2-en-1-yl]-24-phenyl-10,26-dioxa-8,15,24,31-tetraazaundecacyclo[29.5.2.0^{1,32}.0^{2,7}.0^{8,36}.0^{9,22}.0^{13,21}.0^{15,19}.0^{18,23}.0^{25,35}.0^{29,34}]octatriaconta-2,4,6,12,28-pentaene-15,31-diium dibromide
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C46H56Br2N4O2
 1
1
IC50 > 100000 nM
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CP0633849
(1S,11S,13S,17R,18R,20R,27S,29R,30R,31S,35E)-14,26-bis(cyclohex-2-en-1-yl)-35-(2-hydroxyethylidene)-19-phenyl-21-oxa-8,14,19,26-tetraazadecacyclo[24.5.2.2^{11,14}.0^{1,27}.0^{2,7}.0^{8,31}.0^{10,18}.0^{13,17}.0^{20,30}.0^{24,29}]pentatriaconta-2,4,6,9,23-pentaene-14,26-bis(ylium) dibromide
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C50H60Br2N4O2
 1
1
IC50 > 100000 nM
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CP0633850
trimethyl({20-[(trimethylazaniumyl)methyl]-3,13-diazapentacyclo[11.7.0.0^{3,11}.0^{4,9}.0^{14,19}]icosa-1(20),4,6,8,10,14(19),15,17-octaen-10-yl}methyl)azanium diiodide
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C26H34I2N4
 1
1
IC50 > 100000 nM
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CP0633851
(1S,11S,13S,18R,20R,27S,29R,30R,31S,35E)-35-(2-hydroxyethylidene)-14,26-bis[(4-nitrophenyl)methyl]-19-phenyl-21-oxa-8,14,19,26-tetraazadecacyclo[24.5.2.2^{11,14}.0^{1,27}.0^{2,7}.0^{8,31}.0^{10,18}.0^{13,17}.0^{20,30}.0^{24,29}]pentatriaconta-2,4,6,9,23-pentaene-14,26-diium dibromide
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C52H54Br2N6O6
 1
1
IC50 > 100000 nM
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CP0633852
2-[(1R,11S,13S,17S,18R,20R,27S,29R,30R,31S,35E)-19-phenyl-21-oxa-8,14,19,26-tetraazadecacyclo[24.5.2.2^{11,14}.0^{1,27}.0^{2,7}.0^{8,31}.0^{10,18}.0^{13,17}.0^{20,30}.0^{24,29}]pentatriaconta-2,4,6,9,23-pentaen-35-ylidene]ethan-1-ol
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C38H42N4O2
 1
1
IC50 > 100000 nM
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CP0634165
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-dimethyl-24-phenyl-10,26-dioxa-8,15,24,31-tetraazaundecacyclo[29.5.2.0^{1,32}.0^{2,7}.0^{8,36}.0^{9,22}.0^{13,21}.0^{15,19}.0^{18,23}.0^{25,35}.0^{29,34}]octatriaconta-2,4,6,12,28-pentaene-15,31-diium diiodide
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C40H48I2N4O2
 1
1
IC50 > 100000 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0003097
CHEBI:28973
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C21H22N2O2
 2
1 IC50 = 27 nM
2 IC50 = 134 nM
CP0012887
N-[(4aR,5aS,8aR,13aS,15aS,15bR)-14-oxo-4a,5,5a,7,8,13a,15,15a,15b,16-decahydro-2H-4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-10-yl]-11-[3-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[3-[[11-[[(4aR,5aS,8aR,13aS,15aS,15bR)-14-oxo-4a,5,5a,7,8,13a,15,15a,15b,16-decahydro-2H-4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinolin-10-yl]amino]-11-oxoundecyl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoylamino]undecanamide
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C92H138N8O20
 2
1 IC50 = 67 nM
2 IC50 = 3312 nM
Clinical Information about the Protein
Target 1 ( Strychnine-binding glycine receptor (GLRA1) )
Target Type Successful Target
Disease 2 Target-related Diseases  2
1 Muscle spasm [ICD-11: MB47.3]
2 Sepsis [ICD-11: 1G40-1G41]
Approved Drug(s) 1 Approved Drug  1
1 THIOCOLCHICOSIDE Approved
Muscle spasm
Discontinued Drug(s) 1 Discontinued Drug  1
1 GINKOLIDE B Terminated
Sepsis