| Reaction Details |
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 | Report a problem with these data |
| Target | Inhibitor of nuclear factor kappa-B kinase subunit alpha |
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| Ligand | BDBM25919 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_699029 (CHEMBL1646310) |
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| IC50 | 7000±n/a nM |
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| Citation |  Dyckman, AJ; Langevine, CM; Quesnelle, C; Kempson, J; Guo, J; Gill, P; Spergel, SH; Watterson, SH; Li, T; Nirschl, DS; Gillooly, KM; Pattoli, MA; McIntyre, KW; Chen, L; McKinnon, M; Dodd, JH; Barrish, JC; Burke, JR; Pitts, WJ Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis. Bioorg Med Chem Lett21:383-6 (2010) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Inhibitor of nuclear factor kappa-B kinase subunit alpha |
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| Name: | Inhibitor of nuclear factor kappa-B kinase subunit alpha |
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| Synonyms: | CHUK | Conserved helix-loop-helix ubiquitous kinase | I-kappa-B kinase 1 | I-kappa-B kinase alpha | IKK-A | IKK-alpha | IKK1 | IKK2/IKK1 | IKKA | IKKA_HUMAN | IkBKA | IkappaB kinase | Inhibitor of NF-kappa-B kinase alpha/beta | NFKBIKA | Nuclear factor NF-kappa-B inhibitor kinase alpha | TCF-16 | TCF16 | Transcription factor 16 |
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| Type: | PROTEIN |
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| Mol. Mass.: | 84642.21 |
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| Organism: | Homo sapiens (Human) |
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| Description: | ChEMBL_327453 |
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| Residue: | 745 |
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| Sequence: | MERPPGLRPGAGGPWEMRERLGTGGFGNVCLYQHRELDLKIAIKSCRLELSTKNRERWCH
EIQIMKKLNHANVVKACDVPEELNILIHDVPLLAMEYCSGGDLRKLLNKPENCCGLKESQ
ILSLLSDIGSGIRYLHENKIIHRDLKPENIVLQDVGGKIIHKIIDLGYAKDVDQGSLCTS
FVGTLQYLAPELFENKPYTATVDYWSFGTMVFECIAGYRPFLHHLQPFTWHEKIKKKDPK
CIFACEEMSGEVRFSSHLPQPNSLCSLVVEPMENWLQLMLNWDPQQRGGPVDLTLKQPRC
FVLMDHILNLKIVHILNMTSAKIISFLLPPDESLHSLQSRIERETGINTGSQELLSETGI
SLDPRKPASQCVLDGVRGCDSYMVYLFDKSKTVYEGPFASRSLSDCVNYIVQDSKIQLPI
IQLRKVWAEAVHYVSGLKEDYSRLFQGQRAAMLSLLRYNANLTKMKNTLISASQQLKAKL
EFFHKSIQLDLERYSEQMTYGISSEKMLKAWKEMEEKAIHYAEVGVIGYLEDQIMSLHAE
IMELQKSPYGRRQGDLMESLEQRAIDLYKQLKHRPSDHSYSDSTEMVKIIVHTVQSQDRV
LKELFGHLSKLLGCKQKIIDLLPKVEVALSNIKEADNTVMFMQGKRQKEIWHLLKIACTQ
SSARSLVGSSLEGAVTPQTSAWLPPTSAEHDHSLSCVVTPQDGETSAQMIEENLNCLGHL
STIIHEANEEQGNSMMNLDWSWLTE
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| BDBM25919 |
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| n/a |
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| Name | BDBM25919 |
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| Synonyms: | BMS-345541 | BMS345541 | CHEMBL471496 | N-(2-aminoethyl)-3,12-dimethyl-2,5,8-triazatricyclo[7.4.0.0^{2,6}]trideca-1(13),3,5,7,9,11-hexaen-7-amine |
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| Type | Small organic molecule |
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| Emp. Form. | C14H17N5 |
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| Mol. Mass. | 255.3183 |
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| SMILES | Cc1cnc2c(NCCN)nc3ccc(C)cc3n12 |
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| Structure | 
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