| Reaction Details |
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 | Report a problem with these data |
| Target | G protein-activated inward rectifier potassium channel 1/2 |
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| Ligand | BDBM50437952 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_972869 (CHEMBL2411646) |
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| IC50 | 650±n/a nM |
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| Citation |  Wen, W; Wu, W; Romaine, IM; Kaufmann, K; Du, Y; Sulikowski, GA; Weaver, CD; Lindsley, CW Discovery of 'molecular switches' within a GIRK activator scaffold that afford selective GIRK inhibitors. Bioorg Med Chem Lett23:4562-6 (2013) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| G protein-activated inward rectifier potassium channel 1/2 |
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| Name: | G protein-activated inward rectifier potassium channel 1/2 |
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| Synonyms: | Kir3.1/Kir3.2 |
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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 972869 |
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| Components: | This complex has 2 components. |
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| Component 1 |
| Name: | G protein-activated inward rectifier potassium channel 1 |
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| Synonyms: | GIRK-1 | GIRK1 | Inward rectifier K(+) channel Kir3.1 | KCNJ3 | KCNJ3_HUMAN | Potassium channel, inwardly rectifying subfamily J member 3 |
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| Type: | PROTEIN |
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| Mol. Mass.: | 56610.74 |
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| Organism: | Homo sapiens (Human) |
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| Description: | ChEMBL_107915 |
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| Residue: | 501 |
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| Sequence: | MSALRRKFGDDYQVVTTSSSGSGLQPQGPGQDPQQQLVPKKKRQRFVDKNGRCNVQHGNL
GSETSRYLSDLFTTLVDLKWRWNLFIFILTYTVAWLFMASMWWVIAYTRGDLNKAHVGNY
TPCVANVYNFPSAFLFFIETEATIGYGYRYITDKCPEGIILFLFQSILGSIVDAFLIGCM
FIKMSQPKKRAETLMFSEHAVISMRDGKLTLMFRVGNLRNSHMVSAQIRCKLLKSRQTPE
GEFLPLDQLELDVGFSTGADQLFLVSPLTICHVIDAKSPFYDLSQRSMQTEQFEIVVILE
GIVETTGMTCQARTSYTEDEVLWGHRFFPVISLEEGFFKVDYSQFHATFEVPTPPYSVKE
QEEMLLMSSPLIAPAITNSKERHNSVECLDGLDDITTKLPSKLQKITGREDFPKKLLRMS
STTSEKAYSLGDLPMKLQRISSVPGNSEEKLVSKTTKMLSDPMSQSVADLPPKLQKMAGG
AARMEGNLPAKLRKMNSDRFT
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| Component 2 |
| Name: | G protein-activated inward rectifier potassium channel 2 |
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| Synonyms: | BIR1 | GIRK-2 | GIRK2 | Inward rectifier K(+) channel Kir3.2 | KATP-2 | KATP2 | KCNJ6 | KCNJ6_HUMAN | KCNJ7 | Potassium channel, inwardly rectifying subfamily J member 6 |
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| Type: | PROTEIN |
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| Mol. Mass.: | 48440.73 |
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| Organism: | Homo sapiens (Human) |
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| Description: | ChEMBL_107630 |
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| Residue: | 423 |
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| Sequence: | MAKLTESMTNVLEGDSMDQDVESPVAIHQPKLPKQARDDLPRHISRDRTKRKIQRYVRKD
GKCNVHHGNVRETYRYLTDIFTTLVDLKWRFNLLIFVMVYTVTWLFFGMIWWLIAYIRGD
MDHIEDPSWTPCVTNLNGFVSAFLFSIETETTIGYGYRVITDKCPEGIILLLIQSVLGSI
VNAFMVGCMFVKISQPKKRAETLVFSTHAVISMRDGKLCLMFRVGDLRNSHIVEASIRAK
LIKSKQTSEGEFIPLNQTDINVGYYTGDDRLFLVSPLIISHEINQQSPFWEISKAQLPKE
ELEIVVILEGMVEATGMTCQARSSYITSEILWGYRFTPVLTLEDGFYEVDYNSFHETYET
STPSLSAKELAELASRAELPLSWSVSSKLNQHAELETEEEEKNLEEQTERNGDVANLENE
SKV
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| BDBM50437952 |
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| n/a |
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| Name | BDBM50437952 |
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| Synonyms: | CHEMBL2409118 |
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| Type | Small organic molecule |
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| Emp. Form. | C20H18F2N4O |
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| Mol. Mass. | 368.3799 |
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| SMILES | Fc1ccc(NC(=O)Nc2cc(CC3CC3)nn2-c2ccccc2)cc1F |
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| Structure | 
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