2.1 1-(4-'GHstar'-1H-indol-3-yl)-2-(di'ALK'amino)ethan-1-one

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Date

4 substances in Reaxys

2016-07-23 02h:37m:06s (EST)

ALK N

ALK

O GH*

1. Query

NH

Search as: As drawn, No mixtures, No isotopes, No charges, No radicals

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Reaxys ID 160879 View in Reaxys

1/4 CAS Registry Number: 30256-72-5 Chemical Name: 2-dimethylamino-1-indol-3-yl-ethanone; 2-Dimethylamino-1-indol-3-yl-aethanon; Indolyl-(3)-dimethylaminomethyl-keton; 3-(Dimethylamino-acetyl)-indol Linear Structure Formula: C12H14N2O Molecular Formula: C12H14N2O Molecular Weight: 202.256 Type of Substance: heterocyclic InChI Key: HEQAZZLMFKEHFY-UHFFFAOYSA-N Note:

NH

O

N

Substance Label (2) Label References keto-2C

Celik, Leyla; Sinning, Steffen; Severinsen, Kasper; Hansen, Carsten G.; Moller, Maria S.; Bols, Mikael; Wiborg, Ove; Schiott, Birgit; Journal of the American Chemical Society; vol. 130; nb. 12; (2008); p. 3853 3865, View in Reaxys

II

Preobrazhenskaya,M.N. et al.; Pharmaceutical Chemistry Journal; nb. 10; (1970); p. 532 - 536; KhimikoFarmatsevticheskii Zhurnal; vol. 4; nb. 10; (1970); p. 5 - 9, View in Reaxys

Derivative (2) Comment (Derivative)

References

Pikrat: F: 181-183grad

Bodendorf; Walk; Archiv der Pharmazie und Berichte der Deutschen Pharmazeutischen Gesellschaft; vol. 294; (1961); p. 484,487, View in Reaxys

Hydrochlorid: F: 229grad

Bodendorf; Walk; Archiv der Pharmazie und Berichte der Deutschen Pharmazeutischen Gesellschaft; vol. 294; (1961); p. 484,487, View in Reaxys

Melting Point (5) 1 of 5

Melting Point [°C]

208 - 209

Preobrazhenskaya,M.N. et al.; Pharmaceutical Chemistry Journal; nb. 10; (1970); p. 532 - 536; Khimiko-Farmatsevticheskii Zhurnal; vol. 4; nb. 10; (1970); p. 5 - 9, View in Reaxys 2 of 5

Melting Point [°C]

203 - 205

Noell,C.W.; Cheng,C.C.; Journal of Heterocyclic Chemistry; vol. 3; (1966); p. 5 - 8, View in Reaxys 3 of 5

Melting Point [°C]

208 - 209

Solvent (Melting Point)

ethanol

Bodendorf; Walk; Archiv der Pharmazie und Berichte der Deutschen Pharmazeutischen Gesellschaft; vol. 294; (1961); p. 484,487, View in Reaxys 4 of 5

Melting Point [°C]

209 - 211

Solvent (Melting Point)

ethanol; 2-methoxy-ethanol

Ames et al.; Journal of the Chemical Society; (1956); p. 1984,1988, View in Reaxys 5 of 5

Melting Point [°C]

205 - 208

Solvent (Melting Point)

propan-2-ol

Patent; Upjohn Co.; US2821532; (1955), View in Reaxys Further Information (1) Description (Fur- References ther Information) Further information

Bodendorf; Walk; Archiv der Pharmazie und Berichte der Deutschen Pharmazeutischen Gesellschaft; vol. 294; (1961); p. 484,487, View in Reaxys

IR Spectroscopy (1) 1 of 1

Description (IR Spectroscopy)

Bands

Solvent (IR Spectroscopy)

nujol

Comment (IR Spectroscopy)

3110 - 720 cm**(-1)

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Tanner; Spectrochimica Acta; vol. 9; (1957); p. 282,283, View in Reaxys Pharmacological Data (15) 1 of 15

Comment (Pharmacological Data)

Bioactivities present

Noell,C.W.; Cheng,C.C.; Journal of Heterocyclic Chemistry; vol. 3; (1966); p. 5 - 8, View in Reaxys; Preobrazhenskaya,M.N. et al.; Pharmaceutical Chemistry Journal; nb. 10; (1970); p. 532 - 536; Khimiko-Farmatsevticheskii Zhurnal; vol. 4; nb. 10; (1970); p. 5 - 9, View in Reaxys; Tanner; Spectrochimica Acta; vol. 9; (1957); p. 282,283, View in Reaxys; Ames et al.; Journal of the Chemical Society; (1956); p. 1984,1988, View in Reaxys; Patent; Upjohn Co.; US2821532; (1955), View in Reaxys; Bodendorf; Walk; Archiv der Pharmazie und Berichte der Deutschen Pharmazeutischen Gesellschaft; vol. 294; (1961); p. 484,487, View in Reaxys; Celik, Leyla; Sinning, Steffen; Severinsen, Kasper; Hansen, Carsten G.; Moller, Maria S.; Bols, Mikael; Wiborg, Ove; Schiott, Birgit; Journal of the American Chemical Society; vol. 130; nb. 12; (2008); p. 3853 - 3865, View in Reaxys 2 of 15

Effect (Pharmacological Data)

5-HT uptake; inhibition of

Species or Test-System (Pharmacological Data)

HEK-293 MSR cells transfected with hSERT

Method (Pharmacological Data)

inhibition of <3H>-5-HT uptake assayed; cells preincubated with title comp. for 30 min in PBSCM pH 7.4; uptake initiated by addition of <3H>-5-HT (50-100 nM) and continued for 10 min; cells lysed, radiolabeled 5-HT quantified by scintillation counting

Further Details (Pharmacological Data)

hSERT: human serotonin transporter

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

11.5 μmol/l

Celik, Leyla; Sinning, Steffen; Severinsen, Kasper; Hansen, Carsten G.; Moller, Maria S.; Bols, Mikael; Wiborg, Ove; Schiott, Birgit; Journal of the American Chemical Society; vol. 130; nb. 12; (2008); p. 3853 - 3865, View in Reaxys 3 of 15

Effect (Pharmacological Data)

5-HT uptake; inhibition of

Species or Test-System (Pharmacological Data)

HEK-293 MSR cells transfected with hSERT, Ala173Ser mutant

Method (Pharmacological Data)

inhibition of <3H>-5-HT uptake assayed; cells preincubated with title comp. for 30 min in PBSCM pH 7.4; uptake initiated by addition of <3H>-5-HT (50-100 nM) and continued for 10 min; cells lysed, radiolabeled 5-HT quantified by scintillation counting

Further Details (Pharmacological Data)

hSERT: human serotonin transporter

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

4.9 μmol/l

Celik, Leyla; Sinning, Steffen; Severinsen, Kasper; Hansen, Carsten G.; Moller, Maria S.; Bols, Mikael; Wiborg, Ove; Schiott, Birgit; Journal of the American Chemical Society; vol. 130; nb. 12; (2008); p. 3853 - 3865, View in Reaxys 4 of 15

Effect (Pharmacological Data)

5-HT uptake; inhibition of

Species or Test-System (Pharmacological Data)

HEK-293 MSR cells transfected with hSERT, Thr439Ser mutant

Method (Pharmacological Data)

inhibition of <3H>-5-HT uptake assayed; cells preincubated with title comp. for 30 min in PBSCM pH 7.4; uptake initiated by addition of <3H>-5-HT (50-100 nM) and continued for 10 min; cells lysed, radiolabeled 5-HT quantified by scintillation counting

Further Details (Pharmacological Data)

hSERT: human serotonin transporter

Type (Pharmacological Data)

Ki

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Value of Type (Pharmacological Data)

5.6 μmol/l

Celik, Leyla; Sinning, Steffen; Severinsen, Kasper; Hansen, Carsten G.; Moller, Maria S.; Bols, Mikael; Wiborg, Ove; Schiott, Birgit; Journal of the American Chemical Society; vol. 130; nb. 12; (2008); p. 3853 - 3865, View in Reaxys 5 of 15

Effect (Pharmacological Data)

5-HT uptake; inhibition of

Species or Test-System (Pharmacological Data)

HEK-293 MSR cells transfected with hSERT, Thr439Ala mutant

Method (Pharmacological Data)

inhibition of <3H>-5-HT uptake assayed; cells preincubated with title comp. for 30 min in PBSCM pH 7.4; uptake initiated by addition of <3H>-5-HT (50-100 nM) and continued for 10 min; cells lysed, radiolabeled 5-HT quantified by scintillation counting

Further Details (Pharmacological Data)

hSERT: human serotonin transporter

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

4.2 μmol/l

Celik, Leyla; Sinning, Steffen; Severinsen, Kasper; Hansen, Carsten G.; Moller, Maria S.; Bols, Mikael; Wiborg, Ove; Schiott, Birgit; Journal of the American Chemical Society; vol. 130; nb. 12; (2008); p. 3853 - 3865, View in Reaxys 6 of 15

Effect (Pharmacological Data)

5-HT uptake; inhibition of

Species or Test-System (Pharmacological Data)

HEK-293 MSR cells transfected with hSERT, Tyr176Phe mutant

Method (Pharmacological Data)

inhibition of <3H>-5-HT uptake assayed; cells preincubated with title comp. for 30 min in PBSCM pH 7.4; uptake initiated by addition of <3H>-5-HT (50-100 nM) and continued for 10 min; cells lysed, radiolabeled 5-HT quantified by scintillation counting

Further Details (Pharmacological Data)

hSERT: human serotonin transporter

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

22 μmol/l

Celik, Leyla; Sinning, Steffen; Severinsen, Kasper; Hansen, Carsten G.; Moller, Maria S.; Bols, Mikael; Wiborg, Ove; Schiott, Birgit; Journal of the American Chemical Society; vol. 130; nb. 12; (2008); p. 3853 - 3865, View in Reaxys 7 of 15

Effect (Pharmacological Data)

5-HT uptake; inhibition of

Species or Test-System (Pharmacological Data)

HEK-293 MSR cells transfected with hSERT, Tyr175Phe mutant

Method (Pharmacological Data)

inhibition of <3H>-5-HT uptake assayed; cells preincubated with title comp. for 30 min in PBSCM pH 7.4; uptake initiated by addition of <3H>-5-HT (50-100 nM) and continued for 10 min; cells lysed, radiolabeled 5-HT quantified by scintillation counting

Further Details (Pharmacological Data)

hSERT: human serotonin transporter

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

7.1 μmol/l

Celik, Leyla; Sinning, Steffen; Severinsen, Kasper; Hansen, Carsten G.; Moller, Maria S.; Bols, Mikael; Wiborg, Ove; Schiott, Birgit; Journal of the American Chemical Society; vol. 130; nb. 12; (2008); p. 3853 - 3865, View in Reaxys 8 of 15

Effect (Pharmacological Data)

5-HT uptake; inhibition of

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Species or Test-System (Pharmacological Data)

HEK-293 MSR cells transfected with hSERT, Asp98Glu mutant

Method (Pharmacological Data)

inhibition of <3H>-5-HT uptake assayed; cells preincubated with title comp. for 30 min in PBSCM pH 7.4; uptake initiated by addition of <3H>-5-HT (50-100 nM) and continued for 10 min; cells lysed, radiolabeled 5-HT quantified by scintillation counting

Further Details (Pharmacological Data)

hSERT: human serotonin transporter

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

2.8 μmol/l

Celik, Leyla; Sinning, Steffen; Severinsen, Kasper; Hansen, Carsten G.; Moller, Maria S.; Bols, Mikael; Wiborg, Ove; Schiott, Birgit; Journal of the American Chemical Society; vol. 130; nb. 12; (2008); p. 3853 - 3865, View in Reaxys 9 of 15

Effect (Pharmacological Data)

5-HT uptake; inhibition of

Species or Test-System (Pharmacological Data)

HEK-293 MSR cells transfected with hSERT, Ala173Leu mutant

Method (Pharmacological Data)

inhibition of <3H>-5-HT uptake assayed; cells preincubated with title comp. for 30 min in PBSCM pH 7.4; uptake initiated by addition of <3H>-5-HT (50-100 nM) and continued for 10 min; cells lysed, radiolabeled 5-HT quantified by scintillation counting

Further Details (Pharmacological Data)

hSERT: human serotonin transporter

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

2.7 μmol/l

Celik, Leyla; Sinning, Steffen; Severinsen, Kasper; Hansen, Carsten G.; Moller, Maria S.; Bols, Mikael; Wiborg, Ove; Schiott, Birgit; Journal of the American Chemical Society; vol. 130; nb. 12; (2008); p. 3853 - 3865, View in Reaxys 10 of 15

Effect (Pharmacological Data)

5-HT uptake; inhibition of

Species or Test-System (Pharmacological Data)

HEK-293 MSR cells transfected with hSERT, Ala173Met mutant

Method (Pharmacological Data)

inhibition of <3H>-5-HT uptake assayed; cells preincubated with title comp. for 30 min in PBSCM pH 7.4; uptake initiated by addition of <3H>-5-HT (50-100 nM) and continued for 10 min; cells lysed, radiolabeled 5-HT quantified by scintillation counting

Further Details (Pharmacological Data)

hSERT: human serotonin transporter

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

9.3 μmol/l

Celik, Leyla; Sinning, Steffen; Severinsen, Kasper; Hansen, Carsten G.; Moller, Maria S.; Bols, Mikael; Wiborg, Ove; Schiott, Birgit; Journal of the American Chemical Society; vol. 130; nb. 12; (2008); p. 3853 - 3865, View in Reaxys 11 of 15

Effect (Pharmacological Data)

5-HT uptake; inhibition of

Species or Test-System (Pharmacological Data)

HEK-293 MSR cells transfected with hSERT, Ala173Asp mutant

Method (Pharmacological Data)

inhibition of <3H>-5-HT uptake assayed; cells preincubated with title comp. for 30 min in PBSCM pH 7.4; uptake initiated by addition of <3H>-5-HT (50-100 nM) and continued for 10 min; cells lysed, radiolabeled 5-HT quantified by scintillation counting

Further Details (Pharmacological Data)

hSERT: human serotonin transporter

Copyright © 2016 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.

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Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

3.2 μmol/l

Celik, Leyla; Sinning, Steffen; Severinsen, Kasper; Hansen, Carsten G.; Moller, Maria S.; Bols, Mikael; Wiborg, Ove; Schiott, Birgit; Journal of the American Chemical Society; vol. 130; nb. 12; (2008); p. 3853 - 3865, View in Reaxys 12 of 15

Effect (Pharmacological Data)

5-HT uptake; inhibition of

Species or Test-System (Pharmacological Data)

HEK-293 MSR cells transfected with hSERT, Ala173Thr mutant

Method (Pharmacological Data)

inhibition of <3H>-5-HT uptake assayed; cells preincubated with title comp. for 30 min in PBSCM pH 7.4; uptake initiated by addition of <3H>-5-HT (50-100 nM) and continued for 10 min; cells lysed, radiolabeled 5-HT quantified by scintillation counting

Further Details (Pharmacological Data)

hSERT: human serotonin transporter

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

9.9 μmol/l

Celik, Leyla; Sinning, Steffen; Severinsen, Kasper; Hansen, Carsten G.; Moller, Maria S.; Bols, Mikael; Wiborg, Ove; Schiott, Birgit; Journal of the American Chemical Society; vol. 130; nb. 12; (2008); p. 3853 - 3865, View in Reaxys 13 of 15

Effect (Pharmacological Data)

5-HT uptake; inhibition of

Species or Test-System (Pharmacological Data)

HEK-293 MSR cells transfected with hSERT, Thr439Val mutant

Method (Pharmacological Data)

inhibition of <3H>-5-HT uptake assayed; cells preincubated with title comp. for 30 min in PBSCM pH 7.4; uptake initiated by addition of <3H>-5-HT (50-100 nM) and continued for 10 min; cells lysed, radiolabeled 5-HT quantified by scintillation counting

Further Details (Pharmacological Data)

hSERT: human serotonin transporter

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

3.4 μmol/l

Celik, Leyla; Sinning, Steffen; Severinsen, Kasper; Hansen, Carsten G.; Moller, Maria S.; Bols, Mikael; Wiborg, Ove; Schiott, Birgit; Journal of the American Chemical Society; vol. 130; nb. 12; (2008); p. 3853 - 3865, View in Reaxys 14 of 15

Effect (Pharmacological Data)

5-HT uptake; inhibition of

Species or Test-System (Pharmacological Data)

HEK-293 MSR cells transfected with hSERT, Ala169Ile mutant

Method (Pharmacological Data)

inhibition of <3H>-5-HT uptake assayed; cells preincubated with title comp. for 30 min in PBSCM pH 7.4; uptake initiated by addition of <3H>-5-HT (50-100 nM) and continued for 10 min; cells lysed, radiolabeled 5-HT quantified by scintillation counting

Further Details (Pharmacological Data)

hSERT: human serotonin transporter

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

28 μmol/l

Celik, Leyla; Sinning, Steffen; Severinsen, Kasper; Hansen, Carsten G.; Moller, Maria S.; Bols, Mikael; Wiborg, Ove; Schiott, Birgit; Journal of the American Chemical Society; vol. 130; nb. 12; (2008); p. 3853 - 3865, View in Reaxys

Copyright © 2016 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.

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15 of 15

Effect (Pharmacological Data)

5-HT uptake; inhibition of

Species or Test-System (Pharmacological Data)

HEK-293 MSR cells transfected with hSERT, Ala173Cys mutant

Method (Pharmacological Data)

inhibition of <3H>-5-HT uptake assayed; cells preincubated with title comp. for 30 min in PBSCM pH 7.4; uptake initiated by addition of <3H>-5-HT (50-100 nM) and continued for 10 min; cells lysed, radiolabeled 5-HT quantified by scintillation counting

Further Details (Pharmacological Data)

hSERT: human serotonin transporter

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

5.5 μmol/l

Celik, Leyla; Sinning, Steffen; Severinsen, Kasper; Hansen, Carsten G.; Moller, Maria S.; Bols, Mikael; Wiborg, Ove; Schiott, Birgit; Journal of the American Chemical Society; vol. 130; nb. 12; (2008); p. 3853 - 3865, View in Reaxys

Reaxys ID 178782 View in Reaxys

2/4 CAS Registry Number: 92292-25-6 Chemical Name: 2-diethylamino-1-indol-3-yl-ethanone; 2-Diaethylamino-1-indol-3-yl-aethanon; Indolyl-(3)-diethylaminomethyl-keton; 3-(N,N-Diethylaminoacetyl)-indol Linear Structure Formula: C14H18N2O Molecular Formula: C14H18N2O Molecular Weight: 230.31 Type of Substance: heterocyclic InChI Key: KEFPCGXODAAGLR-UHFFFAOYSA-N Note:

NH

O

N

Substance Label (1) Label References 3a

Mutschler; Winkler; Archiv der Pharmazie; vol. 311; nb. 3; (1978); p. 248 - 255, View in Reaxys

Derivative (2) Comment (Derivative)

References

Hydrochlorid: F: 205-215grad (Zers.)

Mutschler; Winkler; Archiv der Pharmazie; vol. 311; nb. 3; (1978); p. 248 - 255, View in Reaxys

Hydrochlorid: F: 211grad

Bodendorf; Walk; Archiv der Pharmazie und Berichte der Deutschen Pharmazeutischen Gesellschaft; vol. 294; (1961); p. 484,487, View in Reaxys

Melting Point (2) 1 of 2

Melting Point [°C]

136 - 137

Solvent (Melting Point)

ethanol

Bodendorf; Walk; Archiv der Pharmazie und Berichte der Deutschen Pharmazeutischen Gesellschaft; vol. 294; (1961); p. 484,487, View in Reaxys 2 of 2

Melting Point [°C]

139 - 141

Solvent (Melting Point)

propan-2-ol

Patent; Upjohn Co.; US2814625; (1954), View in Reaxys Further Information (1) Description (Fur- References ther Information) Further information

Bodendorf; Walk; Archiv der Pharmazie und Berichte der Deutschen Pharmazeutischen Gesellschaft; vol. 294; (1961); p. 484,487, View in Reaxys

Copyright © 2016 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.

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Reaxys ID 3729326 View in Reaxys

3/4 CAS Registry Number: 66803-54-1 Chemical Name: 2-diethylamino-1-indol-3-yl-ethanone; hydrochloride; 2-Diaethylamino-1-indol-3-yl-aethanon; Hydrochlorid Linear Structure Formula: C14H18N2O*ClH Molecular Formula: C14H18N2O*ClH Molecular Weight: 266.771 Type of Substance: heterocyclic InChI Key: MQDQTSUDVCFYJG-UHFFFAOYSA-N Note:

NH

O

Cl

N

H

Melting Point (1) 1 of 1

Melting Point [°C]

213 - 215

Solvent (Melting Point)

propan-2-ol; ethyl acetate

Patent; Upjohn Co.; US2814625; (1954), View in Reaxys

Reaxys ID 3870131 View in Reaxys

4/4 CAS Registry Number: 101721-70-4 Chemical Name: 2-dimethylamino-1-indol-3-yl-ethanone; picrate; 2-Dimethylamino-1-indol-3-yl-aethanon; Picrat Linear Structure Formula: C12H14N2O*C6H3N3O7 Molecular Formula: C6H3N3O7*C12H14N2O Molecular Weight: 431.362 Type of Substance: heterocyclic InChI Key: JCEYYFUTVZHUIK-UHFFFAOYSA-N Note:

O O

NH

N O

HO

N O

O

O

N

N

O

Melting Point (1) 1 of 1

Melting Point [°C]

182 - 184

Solvent (Melting Point)

ethanol

Comment (Melting Point)

Decomp.

Ames et al.; Journal of the Chemical Society; (1956); p. 1984,1988, View in Reaxys Crystal Property Description (1) Colour & Other References Properties gelb

Ames et al.; Journal of the Chemical Society; (1956); p. 1984,1988, View in Reaxys

Copyright © 2016 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.

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