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Glycine receptor subunit alpha-1 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
(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-trioneIC501700.0 [1], 2400.0 [2], 2511.89 [3], 5011.87 [4], 5900.0 [5]
StrychnineIC5051.0 [1], 93.0 [2]
StrychnineKi23.0 [1]
Ginkgolide-BIC501700.0 [1], 1995.26 [2], 3162.28 [3]
Ginkgolide AIC50630.96 [1], 1995.26 [2], 3800.0 [3]
Ginkgolide MIC50501.19 [1], 650.0 [2], 794.33 [3]
(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-oneIC50109.0 [1], 110.0 [2]
(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-oneKi241.0 [1]
(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-oneIC5049.0 [1], 95.0 [2]
(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-oneKi370.0 [1]
(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-oneIC5075.0 [1], 100.0 [2]
(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-oneKi189.0 [1]
Strychnine, 2-propionamido-IC50201.0 [1], 540.0 [2]
Strychnine, 2-propionamido-Ki67.0 [1]
(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-trioneIC503981.07 [1], 6400.0 [2], 7943.28 [3]
(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-oneIC5082.0 [1], 97.0 [2]
(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-oneKi40.0 [1]
(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;bromideIC504590.0 [1], 10000.0 [2]
(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-oneIC5052.0 [1], 59.0 [2]
(1R,3R,6R,7S,8S,9S,10R,11R,12R,13S,16S,17R)-8-Tert-butyl-9-chloro-6,12,17-trihydroxy-16-methyl-2,4,14,18-tetraoxahexacyclo[8.7.2.01,11.03,7.07,11.013,17]nonadecane-5,15,19-trioneIC503162.28 [1], 7943.28 [2]
(1R,3R,6R,7S,8S,9S,10S,11R,12R,13S,16S,17R)-9-Azido-8-tert-butyl-6,12,17-trihydroxy-16-methyl-2,4,14,18-tetraoxahexacyclo[8.7.2.01,11.03,7.07,11.013,17]nonadecane-5,15,19-trioneIC507943.28 [1], 15848.93 [2]
(6R,8S,11S,16R,17S)-8-Tert-butyl-6,16,17-trihydroxy-16-methyl-2,4,14,19-tetraoxahexacyclo[8.7.2.01,11.03,7.07,11.013,17]nonadecane-5,15,18-trioneIC50100000.0 [1]
(1S,8S,11S,13S,16S,17R)-8-Tert-butyl-17-hydroxy-16-methyl-2,4,14,19-tetraoxahexacyclo[8.7.2.01,11.03,7.07,11.013,17]nonadecane-5,6,15,18-tetroneIC50100000.0 [1]
10-Acetoxy-ginkgolide BIC50100000.0 [1]
[(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] acetateIC50100000.0 [1]
10-Methoxymethyloxy-ginkgolide AIC50100000.0 [1]
(1S,6R,8S,9R,11S)-8-Tert-butyl-6,9-dihydroxy-16-methyl-2,4,14,19-tetraoxahexacyclo[8.7.2.01,11.03,7.07,11.013,17]nonadeca-12,16-diene-5,15,18-trioneIC50100000.0 [1]
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-methoxyacetateIC50100000.0 [1]
(1R,2R,3S,6S,8S,10R,11R)-10-Tert-butyl-2,11,16-trihydroxy-3-methyl-5,13,15-trioxapentacyclo[7.5.2.01,8.02,6.08,12]hexadecane-4,14-dioneIC50100000.0 [1]
(1S,2R,3S,6S,8S,10R)-10-Tert-butyl-2-hydroxy-3-methyl-5,13,15-trioxapentacyclo[7.5.2.01,8.02,6.08,12]hexadecane-4,14,16-trioneIC50100000.0 [1]
[(1R,6R,8S,11R)-8-Tert-butyl-13-methoxy-5,15,16-trioxo-2,4,14,17-tetraoxapentacyclo[8.5.2.01,11.03,7.07,11]heptadecan-6-yl] acetateIC50100000.0 [1]
(1R,6R,8S,11S)-8-Tert-butyl-6,13-dimethoxy-2,4,14,17-tetraoxapentacyclo[8.5.2.01,11.03,7.07,11]heptadecane-5,15,16-trioneIC50100000.0 [1]
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]propanoateIC50100000.0 [1]
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]propanoateIC50100000.0 [1]
(1S,6R,8S,11S,13R,16R,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-5,18-dioneIC50100000.0 [1]
(1S,6R,8S,11S,13S,16R,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]nonadecan-18-oneIC50100000.0 [1]
(1R,6R,8S,11S,13S,16R,17R)-8-Tert-butyl-16-methyl-2,4,14,19-tetraoxahexacyclo[8.7.2.01,11.03,7.07,11.013,17]nonadecane-6,17-diolIC50100000.0 [1]
(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[8.7.2.01,11.03,7.07,11.013,17]nonadecane-5,15,18-trioneIC50100000.0 [1]
(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[8.7.2.01,11.03,7.07,11.013,17]nonadecane-5,15,18-trioneIC50100000.0 [1]
[(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[8.7.2.01,11.03,7.07,11.013,17]nonadecan-9-yl] 2-phenylacetateIC50100000.0 [1]
(1S,6R,8S,9S,11R,12R,13S,16S,17R)-8-Tert-butyl-6,9,12,17-tetrahydroxy-16-methyl-2,4,14,19-tetraoxahexacyclo[8.7.2.01,11.03,7.07,11.013,17]nonadecane-5,15,18-trioneIC50100000.0 [1]
[(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[8.7.2.01,11.03,7.07,11.013,17]nonadecan-9-yl] acetateIC50100000.0 [1]
(1S,6R,8S,11R,12R,13S,16S,17R)-8-Tert-butyl-6,12,17-trihydroxy-16-methyl-2,4,14,19-tetraoxahexacyclo[8.7.2.01,11.03,7.07,11.013,17]nonadecane-5,9,15,18-tetroneIC50100000.0 [1]
[(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[8.7.2.01,11.03,7.07,11.013,17]nonadecan-9-yl] trifluoromethanesulfonateIC50100000.0 [1]
(3S,8R,12R,16S,17R,21S)-3-Tert-butyl-17-hydroxy-16-methyl-6,9,11,14,20,22-hexaoxaheptacyclo[10.8.1.15,18.04,8.04,21.013,17.018,21]docosane-7,15,19-trioneIC507943.28 [1], 12589.25 [2]
3,14-Didehydroginkgolide AIC503162.28 [1], 6309.57 [2]
10-Methoxy-ginkgolide CIC505011.87 [1], 10000.0 [2]
(1R,3R,6R,7S,8S,9S,10R,11R,12R,13S,16S,17R)-8-Tert-butyl-9-fluoro-6,12,17-trihydroxy-16-methyl-2,4,14,18-tetraoxahexacyclo[8.7.2.01,11.03,7.07,11.013,17]nonadecane-5,15,19-trioneIC503162.28 [1], 7943.28 [2]
2-AminostrychnineIC5076.0 [1], 77.0 [2]
AlcuroniumIC50100000.0 [1]
Trimethyl-[[20-[(trimethylazaniumyl)methyl]-3,13-diazapentacyclo[11.7.0.03,11.04,9.014,19]icosa-1(20),4,6,8,10,14,16,18-octaen-10-yl]methyl]azanium;diiodideIC50100000.0 [1]
5-Hydroxy-4-[(Z)-indol-3-ylidenemethyl]-3-methyl-1H-imidazol-2-oneIC508800.0 [1]
5-[(1H-Indol-3-yl)methylidene]-1,3-dimethylimidazolidine-2,4-dioneIC50200000.0 [1]
(4Ar,5aS,8aR,13aS,15E,15aR,15bR)-15-(2-phenylethoxyimino)-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-oneIC50690.0 [1]
(4Ar,5aS,8aR,13aS,15E,15aR,15bR)-15-(2-methylpropoxyimino)-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-oneIC50260.0 [1]
Methyl 5-[(E)-[(4aR,5aS,8aR,13aS,15aR,15bR)-14-oxo-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-15-ylidene]amino]oxypentanoateIC50720.0 [1]
(4Ar,5aS,8aR,13aS,15E,15aR,15bR)-15-phenylmethoxyimino-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-oneIC50170.0 [1]
(4Ar,5aS,8aR,13aS,15E,15aR,15bR)-15-pentoxyimino-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-oneIC50250.0 [1]
Methyl 2-[(E)-[(4aR,5aS,8aR,13aS,15aR,15bR)-14-oxo-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-15-ylidene]amino]oxyacetateIC50220.0 [1]
(4Ar,5aS,8aR,13aS,15E,15aR,15bR)-15-butoxyimino-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-oneIC50370.0 [1]
CID 145948364IC5025900.0 [1]
(1R,9R,18S,19S,21R,22R,23R,25R,32S,34R,35R,36S)-24-Phenyl-10,26-dioxa-8,15,24,31-tetrazaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneIC50100000.0 [1]
(2E)-2-[(1R,9Z,11S,13S,17S,18R,20R,27S,29R,30R,31S)-19-Phenyl-21-oxa-8,14,19,26-tetrazadecacyclo[24.5.2.211,14.01,27.02,7.08,31.010,18.013,17.020,30.024,29]pentatriaconta-2,4,6,9,23-pentaen-35-ylidene]ethanolIC50100000.0 [1]
(4Ar,5aS,8aR,13aS,15aS,15bR)-2,4a,5,5a,8,13a,15,15a,15b,16-decahydro4,6-methanoindolo[3,2,1-ij]oxepino[2,3,4-de]pyrrolo[2,3-h]quinoline-7,14-dioneIC506900.0 [1]
[20-[[Dimethyl-[(4-nitrophenyl)methyl]azaniumyl]methyl]-3,13-diazapentacyclo[11.7.0.03,11.04,9.014,19]icosa-1(20),4,6,8,10,14,16,18-octaen-10-yl]methyl-dimethyl-[(4-nitrophenyl)methyl]azaniumIC50100000.0 [1]
[20-[[Dimethyl(prop-2-enyl)azaniumyl]methyl]-3,13-diazapentacyclo[11.7.0.03,11.04,9.014,19]icosa-1(20),4,6,8,10,14,16,18-octaen-10-yl]methyl-dimethyl-prop-2-enylazaniumIC50100000.0 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Dimethyl-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneIC50100000.0 [1]
(1R,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-24-Phenyl-15-prop-2-enyl-10,26-dioxa-8,24,31-triaza-15-azoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneIC50100000.0 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-24-Phenyl-15,31-bis(prop-2-enyl)-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneIC50100000.0 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Bis[(E)-but-2-enyl]-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneIC50100000.0 [1]
2-[(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-31-(2-Acetyloxyethyl)-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaen-15-yl]ethyl acetateIC50100000.0 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Di(cyclohex-2-en-1-yl)-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneIC50100000.0 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Dibenzyl-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneIC50100000.0 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Bis[(3,4-dimethoxyphenyl)methyl]-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneIC50100000.0 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Bis[(4-bromophenyl)methyl]-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneIC50100000.0 [1]
(1S,9R,18R,19S,21R,22R,23R,25R,32S,34R,35R,36S)-15,31-Bis[(4-nitrophenyl)methyl]-24-phenyl-10,26-dioxa-8,24-diaza-15,31-diazoniaundecacyclo[29.5.2.01,32.02,7.08,36.09,22.013,21.015,19.018,23.025,35.029,34]octatriaconta-2,4,6,12,28-pentaeneIC50100000.0 [1]
(2E)-2-[(1S,9Z,11S,13S,17R,18R,20R,27S,29R,30R,31S)-14,26-Dimethyl-19-phenyl-21-oxa-8,19-diaza-14,26-diazoniadecacyclo[24.5.2.211,14.01,27.02,7.08,31.010,18.013,17.020,30.024,29]pentatriaconta-2,4,6,9,23-pentaen-35-ylidene]ethanolIC50100000.0 [1]
(2E)-2-[(1S,9Z,11S,13S,17R,18R,20R,27S,29R,30R,31S)-14,26-Di(cyclohex-2-en-1-yl)-19-phenyl-21-oxa-8,19-diaza-14,26-diazoniadecacyclo[24.5.2.211,14.01,27.02,7.08,31.010,18.013,17.020,30.024,29]pentatriaconta-2,4,6,9,23-pentaen-35-ylidene]ethanolIC50100000.0 [1]
(2E)-2-[(1S,9Z,11S,13S,17R,18R,20R,27S,29R,30R,31S)-14,26-Bis[(3,4-dimethoxyphenyl)methyl]-19-phenyl-21-oxa-8,19-diaza-14,26-diazoniadecacyclo[24.5.2.211,14.01,27.02,7.08,31.010,18.013,17.020,30.024,29]pentatriaconta-2,4,6,9,23-pentaen-35-ylidene]ethanolIC50100000.0 [1]
(2E)-2-[(1S,9Z,11S,13S,18R,20R,27S,29R,30R,31S)-14,26-Bis[(4-nitrophenyl)methyl]-19-phenyl-21-oxa-8,19-diaza-14,26-diazoniadecacyclo[24.5.2.211,14.01,27.02,7.08,31.010,18.013,17.020,30.024,29]pentatriaconta-2,4,6,9,23-pentaen-35-ylidene]ethanolIC50100000.0 [1]
(2E)-2-[(1S,9Z,11S,13S,25Z,27S,33S,35S,36S,38E)-38-(2-Hydroxyethylidene)-14,30-dimethyl-8,24-diaza-14,30-diazoniaundecacyclo[25.5.2.211,14.11,26.110,17.02,7.013,17.018,23.030,33.08,35.024,36]octatriaconta-2,4,6,9,18,20,22,25-octaen-28-ylidene]ethanolIC50100000.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Glycine receptor subunit alpha-1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Dec2024https://www.aatbio.com/data-sets/glycine-receptor-subunit-alpha-1-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024December 21). Quest Database™ Glycine receptor subunit alpha-1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/glycine-receptor-subunit-alpha-1-inhibitors-ic50-ki.
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