Ki Summary

Reaction Details

Report a problem with these data

Target

Gamma-aminobutyric acid receptor subunit alpha-6/beta-2/gamma-2

Ligand

BDBM26263

Substrate

n/a

Meas. Tech.

ChEMBL_217785 (CHEMBL824046)

17±n/a nM

Citation

Wieland, HA; Lüddens, H Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor. J Med Chem 37:4576-80 (1995) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Target

Name:

Gamma-aminobutyric acid receptor subunit alpha-6/beta-2/gamma-2

Synonyms:

GABA A receptor alpha-6/beta-2/gamma-2 | GABA receptor alpha-6/beta-2/gamma-2 subunit

Type:

n/a

Mol. Mass.:

n/a

Description:

ASSAY_ID of EBI is 70244

Components:

This complex has 3 components.

Component 1

Name:

Gamma-aminobutyric acid receptor subunit alpha-6

Synonyms:

Type:

Enzyme Catalytic Domain

Mol. Mass.:

51188.24

Organism:

RAT

Description:

GABA A Alpha6Beta2Gamma2 0 RAT::P30191

Residue:

453

Sequence:

MLLLLPWLFSLLWIENAQAQLEDEGNFYSENVSRILDNLLEGYDNRLRPGFGGAVTEVKTDIYVTSFGPVSDVEMEYTMDVFFRQTWTDERLKFKGPAEILSLNNLMVSKIWTPDTFFRNGKKSIAHNMTTPNKLFRLMHNGTILYTMRLTINADCPMRLVNFPMDGHACPLKFGSYAYPKSEIIYTWKKGPLYSVEVPEESSSLLQYDLIGQTVSSETIKSNTGEYVIMTVYFHLQRKMGYFMIQIYTPCIMTVILSQVSFWINKESVPARTVFGITTVLTMTTLSISARHSLPKVSYATAMDWFIAVCFAFVFSALIEFAAVNYFTNLQSQKAERQAQTAAKPPVAKSKTTESLEAEIVVHSDSKYHLKKRISSLTLPIVPSSEASKVLSRTPILPSTPVTPPLLLPAIGGTSKIDQYSRILFPVAFAGFNLVYWIVYLSKDTMEVSSTVE

Component 2

Name:

Gamma-aminobutyric acid receptor subunit beta-2

Synonyms:

GBRB2_RAT | Gabrb-2 | Gabrb2 | Gamma-aminobutyric acid receptor subunit beta-2 (GABA(A) beta-2)

Type:

Enzyme

Mol. Mass.:

54648.97

Organism:

Rattus norvegicus (Rat)

Description:

P63138

Residue:

474

Sequence:

MWRVRKRGYFGIWSFPLIIAAVCAQSVNDPSNMSLVKETVDRLLKGYDIRLRPDFGGPPVAVGMNIDIASIDMVSEVNMDYTLTMYFQQAWRDKRLSYNVIPLNLTLDNRVADQLWVPDTYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIESYGYTTDDIEFYWRGDDNAVTGVTKIELPQFSIVDYKLITKKVVFSTGSYPRLSLSFKLKRNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIPYVKAIDMYLMGCFVFVFMALLEYALVNYIFFGRGPQRQKKAAEKAANANNEKMRLDVNKMDPHENILLSTLEIKNEMATSEAVMGLGDPRSTMLAYDASSIQYRKAGLPRHSFGRNALERHVAQKKSRLRRRASQLKITIPDLTDVNAIDRWSRIFFPVVFSFFNIVYWLYYVN

Component 3

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:

MSSPNTWSTGSTVYSPVFSQKMTLWILLLLSLYPGFTSQKSDDDYEDYASNKTWVLTPKVPEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQTWYDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLYTLRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQFSFVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDAVPARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFVSNRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCCFEDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL

Inhibitor

Name:

BDBM26263

Synonyms:

Anexate | CHEMBL407 | FLUMAZENIL | Ro15-1788 | Romazicon | [3H]Ro15-1788 | ethyl 12-fluoro-8-methyl-9-oxo-2,4,8-triazatricyclo[8.4.0.0^{2,6}]tetradeca-1(14),3,5,10,12-pentaene-5-carboxylate

Type:

Small organic molecule

Emp. Form.:

C15H14FN3O3

Mol. Mass.:

303.2884

SMILES:

CCOC(=O)c1ncn-2c1CN(C)C(=O)c1cc(F)ccc-21

Structure: