| Reaction Details |
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 | Report a problem with these data |
| Target | Cyclin-dependent kinase 12 |
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| Ligand | BDBM50588263 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2186598 (CHEMBL5098680) |
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| IC50 | 40±n/a nM |
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| Citation |  Barlaam, B; De Savi, C; Dishington, A; Drew, L; Ferguson, AD; Ferguson, D; Gu, C; Hande, S; Hassall, L; Hawkins, J; Hird, AW; Holmes, J; Lamb, ML; Lister, AS; McGuire, TM; Moore, JE; O'Connell, N; Patel, A; Pike, KG; Sarkar, U; Shao, W; Stead, D; Varnes, JG; Vasbinder, MM; Wang, L; Wu, L; Xue, L; Yang, B; Yao, T Discovery of a Series of 7-Azaindoles as Potent and Highly Selective CDK9 Inhibitors for Transient Target Engagement. J Med Chem64:15189-15213 (2021) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Cyclin-dependent kinase 12 |
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| Name: | Cyclin-dependent kinase 12 |
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| Synonyms: | 2.7.11.22 | 2.7.11.23 | CDC2-related protein kinase 7 | CDK12 | CDK12_HUMAN | CRK7 | CRKRS | Cdc2-related kinase, arginine/serine-rich | Cell division cycle 2-related protein kinase 7 | Cell division protein kinase 12 | Cyclin-dependent kinase 12 | KIAA0904 | hCDK12 |
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| Type: | PROTEIN |
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| Mol. Mass.: | 164218.64 |
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| Organism: | Homo sapiens |
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| Description: | ChEMBL_117739 |
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| Residue: | 1490 |
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| Sequence: | MPNSERHGGKKDGSGGASGTLQPSSGGGSSNSRERHRLVSKHKRHKSKHSKDMGLVTPEA
ASLGTVIKPLVEYDDISSDSDTFSDDMAFKLDRRENDERRGSDRSDRLHKHRHHQHRRSR
DLLKAKQTEKEKSQEVSSKSGSMKDRISGSSKRSNEETDDYGKAQVAKSSSKESRSSKLH
KEKTRKERELKSGHKDRSKSHRKRETPKSYKTVDSPKRRSRSPHRKWSDSSKQDDSPSGA
SYGQDYDLSPSRSHTSSNYDSYKKSPGSTSRRQSVSPPYKEPSAYQSSTRSPSPYSRRQR
SVSPYSRRRSSSYERSGSYSGRSPSPYGRRRSSSPFLSKRSLSRSPLPSRKSMKSRSRSP
AYSRHSSSHSKKKRSSSRSRHSSISPVRLPLNSSLGAELSRKKKERAAAAAAAKMDGKES
KGSPVFLPRKENSSVEAKDSGLESKKLPRSVKLEKSAPDTELVNVTHLNTEVKNSSDTGK
VKLDENSEKHLVKDLKAQGTRDSKPIALKEEIVTPKETETSEKETPPPLPTIASPPPPLP
TTTPPPQTPPLPPLPPIPALPQQPPLPPSQPAFSQVPASSTSTLPPSTHSKTSAVSSQAN
SQPPVQVSVKTQVSVTAAIPHLKTSTLPPLPLPPLLPGDDDMDSPKETLPSKPVKKEKEQ
RTRHLLTDLPLPPELPGGDLSPPDSPEPKAITPPQQPYKKRPKICCPRYGERRQTESDWG
KRCVDKFDIIGIIGEGTYGQVYKAKDKDTGELVALKKVRLDNEKEGFPITAIREIKILRQ
LIHRSVVNMKEIVTDKQDALDFKKDKGAFYLVFEYMDHDLMGLLESGLVHFSEDHIKSFM
KQLMEGLEYCHKKNFLHRDIKCSNILLNNSGQIKLADFGLARLYNSEESRPYTNKVITLW
YRPPELLLGEERYTPAIDVWSCGCILGELFTKKPIFQANLELAQLELISRLCGSPCPAVW
PDVIKLPYFNTMKPKKQYRRRLREEFSFIPSAALDLLDHMLTLDPSKRCTAEQTLQSDFL
KDVELSKMAPPDLPHWQDCHELWSKKRRRQRQSGVVVEEPPPSKTSRKETTSGTSTEPVK
NSSPAPPQPAPGKVESGAGDAIGLADITQQLNQSELAVLLNLLQSQTDLSIPQMAQLLNI
HSNPEMQQQLEALNQSISALTEATSQQQDSETMAPEESLKEAPSAPVILPSAEQTTLEAS
STPADMQNILAVLLSQLMKTQEPAGSLEENNSDKNSGPQGPRRTPTMPQEEAAACPPHIL
PPEKRPPEPPGPPPPPPPPPLVEGDLSSAPQELNPAVTAALLQLLSQPEAEPPGHLPHEH
QALRPMEYSTRPRPNRTYGNTDGPETGFSAIDTDERNSGPALTESLVQTLVKNRTFSGSL
SHLGESSSYQGTGSVQFPGDQDLRFARVPLALHPVVGQPFLKAEGSSNSVVHAETKLQNY
GELGPGTTGASSSGAGLHWGGPTQSSAYGKLYRGPTRVPPRGGRGRGVPY
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| BDBM50588263 |
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| n/a |
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| Name | BDBM50588263 |
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| Synonyms: | CHEMBL5198038 |
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| Type | Small organic molecule |
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| Emp. Form. | C24H31N5O2 |
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| Mol. Mass. | 421.5352 |
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| SMILES | CC(C)n1cc(ccc1=O)-c1ccnc2[nH]c(cc12)C1CCN(CC(=O)N(C)C)CC1 |
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| Structure | 
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