Reaction Details |
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Target | Serine/threonine-protein kinase pim-1/pim-2/pim-3 |
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Ligand | BDBM192640 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1622455 (CHEMBL3864807) |
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IC50 | 142±n/a nM |
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Citation | Wurz, RP; Sastri, C; D'Amico, DC; Herberich, B; Jackson, CLM; Pettus, LH; Tasker, AS; Wu, B; Guerrero, N; Lipford, JR; Winston, JT; Yang, Y; Wang, P; Nguyen, Y; Andrews, KL; Huang, X; Lee, MR; Mohr, C; Zhang, JD; Reid, DL; Xu, Y; Zhou, Y; Wang, HL Discovery of imidazopyridazines as potent Pim-1/2 kinase inhibitors. Bioorg Med Chem Lett26:5580-5590 (2016) [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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BDBM192640 |
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n/a |
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Name | BDBM192640 |
Synonyms: | US9187486, 85 |
Type | Small organic molecule |
Emp. Form. | C23H23F2N7 |
Mol. Mass. | 435.4724 |
SMILES | C[C@H]1CC[C@H](N)CN1c1ccncc1Nc1ncc2ccc(nn12)-c1c(F)cccc1F |r| |
Structure |
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