| Reaction Details |
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 | Report a problem with these data |
| Target | Gamma-aminobutyric acid receptor subunit alpha-6/beta-2/delta |
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| Ligand | BDBM50457439 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1759656 (CHEMBL4194664) |
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| IC50 | 150±n/a nM |
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| Citation |  Yakoub, K; Jung, S; Sattler, C; Damerow, H; Weber, J; Kretzschmann, A; Cankaya, AS; Piel, M; Rösch, F; Haugaard, AS; Frølund, B; Schirmeister, T; Lüddens, H Structure-Function Evaluation of Imidazopyridine Derivatives Selective for ?-Subunit-Containing ?-Aminobutyric Acid Type A (GABA J Med Chem61:1951-1968 (2018) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Gamma-aminobutyric acid receptor subunit alpha-6/beta-2/delta |
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| Name: | Gamma-aminobutyric acid receptor subunit alpha-6/beta-2/delta |
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| Synonyms: | n/a |
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| Type: | n/a |
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| Mol. Mass.: | n/a |
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| Description: | ASSAY_ID of ChEMBL is 1759656 |
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| Components: | This complex has 3 components. |
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| Component 1 |
| Name: | Gamma-aminobutyric acid receptor subunit delta |
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| Synonyms: | GABA(A) receptor subunit delta | GBRD_RAT | Gabrd |
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| Type: | Enzyme |
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| Mol. Mass.: | 50571.23 |
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| Organism: | Rattus norvegicus (Rat) |
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| Description: | P18506 |
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| Residue: | 449 |
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| Sequence: | MDVLGWLLLPLLLLCTQPHHGARAMNDIGDYVGSNLEISWLPNLDGLMEGYARNFRPGIG
GPPVNVALALEVASIDHISEANMEYTMTVFLHQSWRDSRLSYNHTNETLGLDSRFVDKLW
LPDTFIVNAKSAWFHDVTVENKLIRLQPDGVILYSIRITSTVACDMDLAKYPMDEQECML
DLESYGYSSEDIVYYWSENQEQIHGLDRLQLAQFTITSYRFTTELMNFKSAGQFPRLSLH
FQLRRNRGVYIIQSYMPSVLLVAMSWVSFWISQAAVPARVSLGITTVLTMTTLMVSARSS
LPRASAIKALDVYFWICYVFVFAALVEYAFAHFNADYRKKRKAKVKVTKPRAEMDVRNAI
VLFSLSAAGVSQELAISRRQGRVPGNLMGSYRSVEVEAKKEGGSRPGGPGGIRSRLKPID
ADTIDIYARAVFPAAFAAVNIIYWAAYTM
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| Component 2 |
| Name: | Gamma-aminobutyric acid receptor subunit alpha-6 |
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| Synonyms: | GABA A Alpha6Beta3Gamma2 | GABA A receptor alpha-6/beta-2/gamma-2 | GABA receptor alpha-6 subunit | GBRA6_RAT | Gabra-6 | Gabra6 | Gamma-aminobutyric acid receptor subunit alpha-6 |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 51188.24 |
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| Organism: | RAT |
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| Description: | GABA A Alpha6Beta2Gamma2 0 RAT::P30191 |
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| Residue: | 453 |
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| Sequence: | MLLLLPWLFSLLWIENAQAQLEDEGNFYSENVSRILDNLLEGYDNRLRPGFGGAVTEVKT
DIYVTSFGPVSDVEMEYTMDVFFRQTWTDERLKFKGPAEILSLNNLMVSKIWTPDTFFRN
GKKSIAHNMTTPNKLFRLMHNGTILYTMRLTINADCPMRLVNFPMDGHACPLKFGSYAYP
KSEIIYTWKKGPLYSVEVPEESSSLLQYDLIGQTVSSETIKSNTGEYVIMTVYFHLQRKM
GYFMIQIYTPCIMTVILSQVSFWINKESVPARTVFGITTVLTMTTLSISARHSLPKVSYA
TAMDWFIAVCFAFVFSALIEFAAVNYFTNLQSQKAERQAQTAAKPPVAKSKTTESLEAEI
VVHSDSKYHLKKRISSLTLPIVPSSEASKVLSRTPILPSTPVTPPLLLPAIGGTSKIDQY
SRILFPVAFAGFNLVYWIVYLSKDTMEVSSTVE
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| Component 3 |
| Name: | Gamma-aminobutyric acid receptor subunit beta-2 |
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| Synonyms: | GBRB2_RAT | Gabrb-2 | Gabrb2 | Gamma-aminobutyric acid receptor subunit beta-2 (GABA(A) beta-2) |
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| Type: | Enzyme |
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| Mol. Mass.: | 54648.97 |
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| Organism: | Rattus norvegicus (Rat) |
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| Description: | P63138 |
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| Residue: | 474 |
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| Sequence: | MWRVRKRGYFGIWSFPLIIAAVCAQSVNDPSNMSLVKETVDRLLKGYDIRLRPDFGGPPV
AVGMNIDIASIDMVSEVNMDYTLTMYFQQAWRDKRLSYNVIPLNLTLDNRVADQLWVPDT
YFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIES
YGYTTDDIEFYWRGDDNAVTGVTKIELPQFSIVDYKLITKKVVFSTGSYPRLSLSFKLKR
NIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIP
YVKAIDMYLMGCFVFVFMALLEYALVNYIFFGRGPQRQKKAAEKAANANNEKMRLDVNKM
DPHENILLSTLEIKNEMATSEAVMGLGDPRSTMLAYDASSIQYRKAGLPRHSFGRNALER
HVAQKKSRLRRRASQLKITIPDLTDVNAIDRWSRIFFPVVFSFFNIVYWLYYVN
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| BDBM50457439 |
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| n/a |
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| Name | BDBM50457439 |
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| Synonyms: | CHEMBL4213357 |
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| Type | Small organic molecule |
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| Emp. Form. | C18H10Br2ClN3OS |
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| Mol. Mass. | 511.618 |
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| SMILES | Clc1ccc(cc1)C(=O)Nc1c(nc2c(Br)cc(Br)cn12)-c1cccs1 |
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| Structure | 
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