Reaction Details |
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Target | Serine/threonine-protein kinase pim-1/pim-2/pim-3 |
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Ligand | BDBM50518504 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1871839 (CHEMBL4373006) |
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EC50 | 70±n/a nM |
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Citation | Barberis, C; Pribish, J; Tserlin, E; Gross, A; Czekaj, M; Barragué, M; Erdman, P; Maniar, S; Jiang, J; Fire, L; Patel, V; Hebert, A; Levit, M; Wang, A; Sun, F; Huang, SA Discovery of N-substituted 7-azaindoles as Pan-PIM kinases inhibitors - Lead optimization - Part III. Bioorg Med Chem Lett29:491-495 (2019) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Serine/threonine-protein kinase pim-1/pim-2/pim-3 |
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Name: | Serine/threonine-protein kinase pim-1/pim-2/pim-3 |
Synonyms: | Serine/threonine-protein kinase PIM |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of ChEMBL is 2135988 |
Components: | This complex has 3 components. |
Component 1 |
Name: | Serine/threonine-protein kinase pim-1 |
Synonyms: | PIM-1 Kinase | PIM1 | PIM1_HUMAN | Proto-oncogene serine/threonine-protein kinase Pim-1 | Serine/threonine-protein kinase (PIM1) | Serine/threonine-protein kinase PIM | Serine/threonine-protein kinase PIM1 | Serine/threonine-protein kinase pim-1 (PIM1) |
Type: | Protein |
Mol. Mass.: | 35681.82 |
Organism: | Homo sapiens (Human) |
Description: | P11309 |
Residue: | 313 |
Sequence: | MLLSKINSLAHLRAAPCNDLHATKLAPGKEKEPLESQYQVGPLLGSGGFGSVYSGIRVSD
NLPVAIKHVEKDRISDWGELPNGTRVPMEVVLLKKVSSGFSGVIRLLDWFERPDSFVLIL
ERPEPVQDLFDFITERGALQEELARSFFWQVLEAVRHCHNCGVLHRDIKDENILIDLNRG
ELKLIDFGSGALLKDTVYTDFDGTRVYSPPEWIRYHRYHGRSAAVWSLGILLYDMVCGDI
PFEHDEEIIRGQVFFRQRVSSECQHLIRWCLALRPSDRPTFEEIQNHPWMQDVLLPQETA
EIHLHSLSPGPSK
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Component 2 |
Name: | Serine/threonine-protein kinase pim-2 |
Synonyms: | PIM2 | PIM2_HUMAN | Pim-2h | Serine/threonine-protein kinase (PIM2) | Serine/threonine-protein kinase PIM | Serine/threonine-protein kinase pim-2 (PIM2) |
Type: | Serine/threonine-protein kinase |
Mol. Mass.: | 34185.93 |
Organism: | Homo sapiens (Human) |
Description: | Q9P1W9 |
Residue: | 311 |
Sequence: | MLTKPLQGPPAPPGTPTPPPGGKDREAFEAEYRLGPLLGKGGFGTVFAGHRLTDRLQVAI
KVIPRNRVLGWSPLSDSVTCPLEVALLWKVGAGGGHPGVIRLLDWFETQEGFMLVLERPL
PAQDLFDYITEKGPLGEGPSRCFFGQVVAAIQHCHSRGVVHRDIKDENILIDLRRGCAKL
IDFGSGALLHDEPYTDFDGTRVYSPPEWISRHQYHALPATVWSLGILLYDMVCGDIPFER
DQEILEAELHFPAHVSPDCCALIRRCLAPKPSSRPSLEEILLDPWMQTPAEDVPLNPSKG
GPAPLAWSLLP
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Component 3 |
Name: | Serine/threonine-protein kinase pim-3 |
Synonyms: | PIM3 | PIM3_HUMAN | Serine/threonine-protein kinase pim-3 (PIM3) |
Type: | Protein |
Mol. Mass.: | 35888.19 |
Organism: | Homo sapiens (Human) |
Description: | Q86V86 |
Residue: | 326 |
Sequence: | MLLSKFGSLAHLCGPGGVDHLPVKILQPAKADKESFEKAYQVGAVLGSGGFGTVYAGSRI
ADGLPVAVKHVVKERVTEWGSLGGATVPLEVVLLRKVGAAGGARGVIRLLDWFERPDGFL
LVLERPEPAQDLFDFITERGALDEPLARRFFAQVLAAVRHCHSCGVVHRDIKDENLLVDL
RSGELKLIDFGSGALLKDTVYTDFDGTRVYSPPEWIRYHRYHGRSATVWSLGVLLYDMVC
GDIPFEQDEEILRGRLLFRRRVSPECQQLIRWCLSLRPSERPSLDQIAAHPWMLGADGGV
PESCDLRLCTLDPDDVASTTSSSESL
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BDBM50518504 |
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n/a |
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Name | BDBM50518504 |
Synonyms: | CHEMBL4466764 |
Type | Small organic molecule |
Emp. Form. | C19H20Cl2N4O3 |
Mol. Mass. | 423.293 |
SMILES | NC(=O)c1cc(Cl)c2c(Cl)c(C#CC3COCCO3)n([C@H]3CCCNC3)c2n1 |r| |
Structure |
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