| Reaction Details |
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 | Report a problem with these data |
| Target | Serine/threonine-protein kinase pim-1/pim-2/pim-3 |
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| Ligand | BDBM238728 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1932814 (CHEMBL4478466) |
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| IC50 | 5760±n/a nM |
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| Citation |  Pettus, LH; Andrews, KL; Booker, SK; Chen, J; Cee, VJ; Chavez, F; Chen, Y; Eastwood, H; Guerrero, N; Herberich, B; Hickman, D; Lanman, BA; Laszlo, J; Lee, MR; Lipford, JR; Mattson, B; Mohr, C; Nguyen, Y; Norman, MH; Powers, D; Reed, AB; Rex, K; Sastri, C; Tamayo, N; Wang, P; Winston, JT; Wu, B; Wu, T; Wurz, RP; Xu, Y; Zhou, Y; Tasker, AS; Wang, HL Discovery and Optimization of Quinazolinone-pyrrolopyrrolones as Potent and Orally Bioavailable Pan-Pim Kinase Inhibitors. J Med Chem59:6407-30 (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 |
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| Synonyms: | Serine/threonine-protein kinase PIM |
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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 2135988 |
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| Components: | This complex has 3 components. |
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| Component 1 |
| Name: | Serine/threonine-protein kinase pim-1 |
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| 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) |
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| Type: | Protein |
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| Mol. Mass.: | 35681.82 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P11309 |
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| Residue: | 313 |
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| Sequence: | MLLSKINSLAHLRAAPCNDLHATKLAPGKEKEPLESQYQVGPLLGSGGFGSVYSGIRVSD
NLPVAIKHVEKDRISDWGELPNGTRVPMEVVLLKKVSSGFSGVIRLLDWFERPDSFVLIL
ERPEPVQDLFDFITERGALQEELARSFFWQVLEAVRHCHNCGVLHRDIKDENILIDLNRG
ELKLIDFGSGALLKDTVYTDFDGTRVYSPPEWIRYHRYHGRSAAVWSLGILLYDMVCGDI
PFEHDEEIIRGQVFFRQRVSSECQHLIRWCLALRPSDRPTFEEIQNHPWMQDVLLPQETA
EIHLHSLSPGPSK
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| Component 2 |
| Name: | Serine/threonine-protein kinase pim-2 |
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| Synonyms: | PIM2 | PIM2_HUMAN | Pim-2h | Serine/threonine-protein kinase (PIM2) | Serine/threonine-protein kinase PIM | Serine/threonine-protein kinase pim-2 (PIM2) |
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| Type: | Serine/threonine-protein kinase |
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| Mol. Mass.: | 34185.93 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q9P1W9 |
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| Residue: | 311 |
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| Sequence: | MLTKPLQGPPAPPGTPTPPPGGKDREAFEAEYRLGPLLGKGGFGTVFAGHRLTDRLQVAI
KVIPRNRVLGWSPLSDSVTCPLEVALLWKVGAGGGHPGVIRLLDWFETQEGFMLVLERPL
PAQDLFDYITEKGPLGEGPSRCFFGQVVAAIQHCHSRGVVHRDIKDENILIDLRRGCAKL
IDFGSGALLHDEPYTDFDGTRVYSPPEWISRHQYHALPATVWSLGILLYDMVCGDIPFER
DQEILEAELHFPAHVSPDCCALIRRCLAPKPSSRPSLEEILLDPWMQTPAEDVPLNPSKG
GPAPLAWSLLP
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| Component 3 |
| Name: | Serine/threonine-protein kinase pim-3 |
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| Synonyms: | PIM3 | PIM3_HUMAN | Serine/threonine-protein kinase pim-3 (PIM3) |
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| Type: | Protein |
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| Mol. Mass.: | 35888.19 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q86V86 |
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| Residue: | 326 |
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| Sequence: | MLLSKFGSLAHLCGPGGVDHLPVKILQPAKADKESFEKAYQVGAVLGSGGFGTVYAGSRI
ADGLPVAVKHVVKERVTEWGSLGGATVPLEVVLLRKVGAAGGARGVIRLLDWFERPDGFL
LVLERPEPAQDLFDFITERGALDEPLARRFFAQVLAAVRHCHSCGVVHRDIKDENLLVDL
RSGELKLIDFGSGALLKDTVYTDFDGTRVYSPPEWIRYHRYHGRSATVWSLGVLLYDMVC
GDIPFEQDEEILRGRLLFRRRVSPECQQLIRWCLSLRPSERPSLDQIAAHPWMLGADGGV
PESCDLRLCTLDPDDVASTTSSSESL
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| BDBM238728 |
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| n/a |
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| Name | BDBM238728 |
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| Synonyms: | US9394297, 409 |
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| Type | Small organic molecule |
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| Emp. Form. | C23H27N5O2 |
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| Mol. Mass. | 405.4928 |
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| SMILES | Cc1nc2cccc(-c3cc4C(=O)NC5(CCOCC5)c4[nH]3)c2nc1NC(C)(C)C |
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| Structure | 
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