Ki Summary

Reaction Details

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Target

Gamma-aminobutyric acid receptor subunit alpha-5/beta-3/gamma-2

Ligand

BDBM50185266

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_343684 (CHEMBL861094)

1500±n/a nM

Citation

Primofiore, G; Da Settimo, F; Marini, AM; Taliani, S; La Motta, C; Simorini, F; Novellino, E; Greco, G; Cosimelli, B; Ehlardo, M; Sala, A; Besnard, F; Montali, M; Martini, C Refinement of the benzodiazepine receptor site topology by structure-activity relationships of new N-(heteroarylmethyl)indol-3-ylglyoxylamides. J Med Chem49:2489-95 (2006) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Gamma-aminobutyric acid receptor subunit alpha-5/beta-3/gamma-2

Name:

Gamma-aminobutyric acid receptor subunit alpha-5/beta-3/gamma-2

Synonyms:

GABA A receptor alpha-5/beta-3/gamma-2 | GABA receptor alpha-5/beta-3/gamma-2 subunit

Type:

n/a

Mol. Mass.:

n/a

Description:

ASSAY_ID of EBI is 70706

Components:

This complex has 3 components.

Component 1

Name:

Gamma-aminobutyric acid receptor subunit gamma-2

Synonyms:

GBRG2_RAT | Gabrg2 | Gamma-aminobutyric acid receptor subunit gamma-2 (GABA(A) gamma-2)

Type:

Enzyme

Mol. Mass.:

54087.63

Organism:

Rattus norvegicus (Rat)

Description:

P18508

Residue:

466

Sequence:

MSSPNTWSTGSTVYSPVFSQKMTLWILLLLSLYPGFTSQKSDDDYEDYASNKTWVLTPKV
PEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQTW
YDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLYT
LRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQFS
FVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDAV
PARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFVS
NRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCCF
EDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL

Component 2

Name:

Gamma-aminobutyric acid receptor subunit alpha-5

Synonyms:

Type:

Enzyme Catalytic Domain

Mol. Mass.:

52350.79

Organism:

RAT

Description:

GABA A alpha5 0 RAT::P19969

Residue:

464

Sequence:

MDNGMLSRFIMTKTLLVFCISMTLSSHFGFSQMPTSSVQDETNDNITIFTRILDGLLDGY
DNRLRPGLGERITQVRTDIYVTSFGPVSDTEMEYTIDVFFRQSWKDERLRFKGPMQRLPL
NNLLASKIWTPDTFFHNGKKSIAHNMTTPNKLLRLEDDGTLLYTMRLTISAECPMQLEDF
PMDAHACPLKFGSYAYPNSEVVYVWTNGSTKSVVVAEDGSRLNQYHLMGQTVGTENISTS
TGEYTIMTAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTM
TTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKKALEAA
KIKKKERELILNKSTNAFTTGKLTHPPNIPKEQLPGGTGNAVGTASIRASEEKTSESKKT
YNSISKIDKMSRIVFPILFGTFNLVYWATYLNREPVIKGATSPK

Component 3

Name:

Gamma-aminobutyric acid receptor subunit beta-3

Synonyms:

GABA receptor beta-3 subunit | GBRB3_RAT | Gabrb-3 | Gabrb3

Type:

PROTEIN

Mol. Mass.:

54180.66

Organism:

Rattus norvegicus

Description:

EBI_12481

Residue:

473

Sequence:

MWGFAGGRLFGIFSAPVLVAVVCCAQSVNDPGNMSFVKETVDKLLKGYDIRLRPDFGGPP
VCVGMNIDIASIDMVSEVNMDYTLTMYFQQYWRDKRLAYSGIPLNLTLDNRVADQLWVPD
TYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIE
SYGYTTDDIEFYWRGGDKAVTGVERIELPQFSIVEHRLVSRNVVFATGAYPRLSLSFRLK
RNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKI
PYVKAIDMYLMGCFVFVFLALLEYAFVNYIFFGRGPQRQKKLAEKTAKAKNDRSKSEINR
VDAHGNILLAPMDVHNEMNEVAGSVGDTRNSAISFDNSGIQYRKQSMPKEGHGRYMGDRS
IPHKKTHLRRRSSQLKIKIPDLTDVNAIDRWSRIVFPFTFSLFNLVYWLYYVN

BDBM50185266

n/a

Name

BDBM50185266

Synonyms:

CHEMBL382882 | N-((1H-pyrrol-2-yl)methyl)-2-(1H-indol-3-yl)-2-oxoacetamide

Type

Small organic molecule

Emp. Form.

C15H13N3O2

Mol. Mass.

267.2826

SMILES

O=C(NCc1ccc[nH]1)C(=O)c1c[nH]c2ccccc12

Structure