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Selective antagonists of mouse trace amine-associated receptor 1 (mTAAR1): Discovery of EPPTB ( RO5212773)
High throughput screening of the Roche compound library identified benzanilides such as 1 and 2 as antagonists of TAAR1. Optimisation of this hit series led to the first selective TAAR1 antagonist ( N-(3-Ethoxy-phenyl)-4-pyrrolidin-1-yl-3-trifluoromethyl-benzamide EPPTB ( RO5212773, 9f) having IC 50...
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| Published in: | Bioorganic & medicinal chemistry letters 2011-02, Vol.21 (4), p.1227-1231 |
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| Main Authors: | , , |
| Format: | Article |
| Language: | English |
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| cited_by | cdi_FETCH-LOGICAL-c507t-ee9b93b38f35c64acf69e21c4f15e99b3c889d7850a55e77357d3d904573bac13 |
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| cites | cdi_FETCH-LOGICAL-c507t-ee9b93b38f35c64acf69e21c4f15e99b3c889d7850a55e77357d3d904573bac13 |
| container_end_page | 1231 |
| container_issue | 4 |
| container_start_page | 1227 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 21 |
| creator | Stalder, Henri Hoener, Marius C. Norcross, Roger D. |
| description | High throughput screening of the Roche compound library identified benzanilides such as
1 and
2 as antagonists of TAAR1. Optimisation of this hit series led to the first selective TAAR1 antagonist (
N-(3-Ethoxy-phenyl)-4-pyrrolidin-1-yl-3-trifluoromethyl-benzamide
EPPTB (
RO5212773,
9f) having IC
50 of 28
nM at mouse TAAR1. |
| doi_str_mv | 10.1016/j.bmcl.2010.12.075 |
| format | article |
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1 and
2 as antagonists of TAAR1. Optimisation of this hit series led to the first selective TAAR1 antagonist (
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EPPTB (
RO5212773,
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50 of 28
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1 and
2 as antagonists of TAAR1. Optimisation of this hit series led to the first selective TAAR1 antagonist (
N-(3-Ethoxy-phenyl)-4-pyrrolidin-1-yl-3-trifluoromethyl-benzamide
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RO5212773,
9f) having IC
50 of 28
nM at mouse TAAR1.</description><subject>Animals</subject><subject>Antagonists</subject><subject>Benzamides - chemical synthesis</subject><subject>Benzamides - chemistry</subject><subject>Benzamides - pharmacology</subject><subject>Benzanilides</subject><subject>Biological and medical sciences</subject><subject>chemistry</subject><subject>Drug Evaluation, Preclinical</subject><subject>EPPTB</subject><subject>High-Throughput Screening Assays</subject><subject>Humans</subject><subject>inhibitory concentration 50</subject><subject>Inverse agonists</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Microsomes, Liver - metabolism</subject><subject>Miscellaneous</subject><subject>Pharmacology. 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1 and
2 as antagonists of TAAR1. Optimisation of this hit series led to the first selective TAAR1 antagonist (
N-(3-Ethoxy-phenyl)-4-pyrrolidin-1-yl-3-trifluoromethyl-benzamide
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RO5212773,
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| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2011-02, Vol.21 (4), p.1227-1231 |
| issn | 0960-894X 1464-3405 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_907150616 |
| source | ScienceDirect Freedom Collection |
| subjects | Animals Antagonists Benzamides - chemical synthesis Benzamides - chemistry Benzamides - pharmacology Benzanilides Biological and medical sciences chemistry Drug Evaluation, Preclinical EPPTB High-Throughput Screening Assays Humans inhibitory concentration 50 Inverse agonists Medical sciences Mice Microsomes, Liver - metabolism Miscellaneous Pharmacology. Drug treatments Protein Binding Pyrrolidines - chemical synthesis Pyrrolidines - chemistry Pyrrolidines - pharmacology Receptors, G-Protein-Coupled - antagonists & inhibitors Receptors, G-Protein-Coupled - metabolism RO5212773 screening Structure-Activity Relationship TAAR1 |
| title | Selective antagonists of mouse trace amine-associated receptor 1 (mTAAR1): Discovery of EPPTB ( RO5212773) |
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