Reaction Details |
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Target | G protein-activated inward rectifier potassium channel 1/4 |
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Ligand | BDBM50437968 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_972874 (CHEMBL2411651) |
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EC50 | 3500±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 1/4 |
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Name: | G protein-activated inward rectifier potassium channel 1/4 |
Synonyms: | GIRK1/4 channels | Kir3.1/Kir3.4 |
Type: | PROTEIN |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 2 components. |
Component 1 |
Name: | G protein-activated inward rectifier potassium channel 1 |
Synonyms: | GIRK-1 | GIRK1 | Inward rectifier K(+) channel Kir3.1 | KCNJ3 | KCNJ3_HUMAN | Potassium channel, inwardly rectifying subfamily J member 3 |
Type: | PROTEIN |
Mol. Mass.: | 56610.74 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_107915 |
Residue: | 501 |
Sequence: | MSALRRKFGDDYQVVTTSSSGSGLQPQGPGQDPQQQLVPKKKRQRFVDKNGRCNVQHGNL
GSETSRYLSDLFTTLVDLKWRWNLFIFILTYTVAWLFMASMWWVIAYTRGDLNKAHVGNY
TPCVANVYNFPSAFLFFIETEATIGYGYRYITDKCPEGIILFLFQSILGSIVDAFLIGCM
FIKMSQPKKRAETLMFSEHAVISMRDGKLTLMFRVGNLRNSHMVSAQIRCKLLKSRQTPE
GEFLPLDQLELDVGFSTGADQLFLVSPLTICHVIDAKSPFYDLSQRSMQTEQFEIVVILE
GIVETTGMTCQARTSYTEDEVLWGHRFFPVISLEEGFFKVDYSQFHATFEVPTPPYSVKE
QEEMLLMSSPLIAPAITNSKERHNSVECLDGLDDITTKLPSKLQKITGREDFPKKLLRMS
STTSEKAYSLGDLPMKLQRISSVPGNSEEKLVSKTTKMLSDPMSQSVADLPPKLQKMAGG
AARMEGNLPAKLRKMNSDRFT
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Component 2 |
Name: | G protein-activated inward rectifier potassium channel 4 |
Synonyms: | CIR | Cardiac inward rectifier | GIRK-4 | GIRK4 | Heart KATP channel | IRK-4 | Inward rectifier K(+) channel Kir3.4 | KATP-1 | KCNJ5 | KCNJ5_HUMAN | Potassium channel, inwardly rectifying subfamily J member 5 |
Type: | PROTEIN |
Mol. Mass.: | 47658.06 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_107914 |
Residue: | 419 |
Sequence: | MAGDSRNAMNQDMEIGVTPWDPKKIPKQARDYVPIATDRTRLLAEGKKPRQRYMEKSGKC
NVHHGNVQETYRYLSDLFTTLVDLKWRFNLLVFTMVYTVTWLFFGFIWWLIAYIRGDLDH
VGDQEWIPCVENLSGFVSAFLFSIETETTIGYGFRVITEKCPEGIILLLVQAILGSIVNA
FMVGCMFVKISQPKKRAETLMFSNNAVISMRDEKLCLMFRVGDLRNSHIVEASIRAKLIK
SRQTKEGEFIPLNQTDINVGFDTGDDRLFLVSPLIISHEINQKSPFWEMSQAQLHQEEFE
VVVILEGMVEATGMTCQARSSYMDTEVLWGHRFTPVLTLEKGFYEVDYNTFHDTYETNTP
SCCAKELAEMKREGRLLQYLPSPPLLGGCAEAGLDAEAEQNEEDEPKGLGGSREARGSV
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BDBM50437968 |
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n/a |
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Name | BDBM50437968 |
Synonyms: | CHEMBL2409134 |
Type | Small organic molecule |
Emp. Form. | C21H21F3N4O |
Mol. Mass. | 402.4128 |
SMILES | CC(C)c1cc(NC(=O)Nc2cccc(c2)C(F)(F)F)n(Cc2ccccc2)n1 |
Structure |
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