General Information of the Protein
Protein ID
PT04296
Protein Name
Cyclin-dependent kinase 12
Secondarily
Protein Name
Cdc2-related kinase
arginine/serine-rich
Cell division cycle 2-related protein kinase 7
Cell division protein kinase 12
Gene Name
CDK12
Secondarily
Gene Name
CRK7
CRKRS
KIAA0904
Sequence
MPNSERHGGKKDGSGGASGTLQPSSGGGSSNSRERHRLVSKHKRHKSKHSKDMGLVTPEAASLGTVIKPLVEYDDISSDSDTFSDDMAFKLDRRENDERRGSDRSDRLHKHRHHQHRRSRDLLKAKQTEKEKSQEVSSKSGSMKDRISGSSKRSNEETDDYGKAQVAKSSSKESRSSKLHKEKTRKERELKSGHKDRSKSHRKRETPKSYKTVDSPKRRSRSPHRKWSDSSKQDDSPSGASYGQDYDLSPSRSHTSSNYDSYKKSPGSTSRRQSVSPPYKEPSAYQSSTRSPSPYSRRQRSVSPYSRRRSSSYERSGSYSGRSPSPYGRRRSSSPFLSKRSLSRSPLPSRKSMKSRSRSPAYSRHSSSHSKKKRSSSRSRHSSISPVRLPLNSSLGAELSRKKKERAAAAAAAKMDGKESKGSPVFLPRKENSSVEAKDSGLESKKLPRSVKLEKSAPDTELVNVTHLNTEVKNSSDTGKVKLDENSEKHLVKDLKAQGTRDSKPIALKEEIVTPKETETSEKETPPPLPTIASPPPPLPTTTPPPQTPPLPPLPPIPALPQQPPLPPSQPAFSQVPASSTSTLPPSTHSKTSAVSSQANSQPPVQVSVKTQVSVTAAIPHLKTSTLPPLPLPPLLPGDDDMDSPKETLPSKPVKKEKEQRTRHLLTDLPLPPELPGGDLSPPDSPEPKAITPPQQPYKKRPKICCPRYGERRQTESDWGKRCVDKFDIIGIIGEGTYGQVYKAKDKDTGELVALKKVRLDNEKEGFPITAIREIKILRQLIHRSVVNMKEIVTDKQDALDFKKDKGAFYLVFEYMDHDLMGLLESGLVHFSEDHIKSFMKQLMEGLEYCHKKNFLHRDIKCSNILLNNSGQIKLADFGLARLYNSEESRPYTNKVITLWYRPPELLLGEERYTPAIDVWSCGCILGELFTKKPIFQANLELAQLELISRLCGSPCPAVWPDVIKLPYFNTMKPKKQYRRRLREEFSFIPSAALDLLDHMLTLDPSKRCTAEQTLQSDFLKDVELSKMAPPDLPHWQDCHELWSKKRRRQRQSGVVVEEPPPSKTSRKETTSGTSTEPVKNSSPAPPQPAPGKVESGAGDAIGLADITQQLNQSELAVLLNLLQSQTDLSIPQMAQLLNIHSNPEMQQQLEALNQSISALTEATSQQQDSETMAPEESLKEAPSAPVILPSAEQTTLEASSTPADMQNILAVLLSQLMKTQEPAGSLEENNSDKNSGPQGPRRTPTMPQEEAAACPPHILPPEKRPPEPPGPPPPPPPPPLVEGDLSSAPQELNPAVTAALLQLLSQPEAEPPGHLPHEHQALRPMEYSTRPRPNRTYGNTDGPETGFSAIDTDERNSGPALTESLVQTLVKNRTFSGSLSHLGESSSYQGTGSVQFPGDQDLRFARVPLALHPVVGQPFLKAEGSSNSVVHAETKLQNYGELGPGTTGASSSGAGLHWGGPTQSSAYGKLYRGPTRVPPRGGRGRGVPY
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
CMGC protein kinase group
>
CMGC protein kinase CDK family
Function
Cyclin-dependent kinase that phosphorylates the C-terminal domain (CTD) of the large subunit of RNA polymerase II (POLR2A), thereby acting as a key regulator of transcription elongation. Regulates the expression of genes involved in DNA repair and is required for the maintenance of genomic stability. Preferentially phosphorylates 'Ser-5' in CTD repeats that are already phosphorylated at 'Ser-7', but can also phosphorylate 'Ser-2'. Required for RNA splicing, possibly by phosphorylating SRSF1/SF2. Involved in regulation of MAP kinase activity, possibly leading to affect the response to estrogen inhibitors.
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Uniprot ID
Primary ID:
Q9NYV4

Secondarily ID:
A7E2B2
B4DYX4
B9EIQ6
O94978
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Ensembl ID
ENSG00000167258
HGNC ID
HGNC:24224
Subcellular Location
Nucleus
Nucleus speckle
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0702758
 Compound Info 
2-(6-(1-acryloylpiperidin-4-yl)pyridin-3-yl)-N-(5-cyclopropyl-1H-pyrazol-3-yl)propanamide
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C22H27N5O2
  1
1
Kd < 25 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0702760
 Compound Info 
(S,E)-N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-(4-(1-(4-(dimethylamino)but-2-enoyl)-1,2,3,6-tetrahydropyridin-4-yl)phenyl)propanamide
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C26H33N5O2
  1
1
Kd < 25 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0767888
 Compound Info 
2-(4-(1-acryloyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl)-N-(5-cyclopropyl-1H-pyrazol-3-yl)propanamide
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C23H26N4O2
  1
1
Kd = 25 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0768164
 Compound Info 
(S)-2-(4-(1-acryloyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl)-N-(5-cyclopropyl-1H-pyrazol-3-yl)propanamide
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C23H26N4O2
  1
1
Kd = 25 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0768165
 Compound Info 
N-(4'-(1-((5-cyclopropyl-1H-pyrazol-3-yl)amino)-1-oxopropan-2-yl)-2,3,4,5-tetrahydro-[1,1-biphenyl]-4-yl)acrylamide
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C24H28N4O2
  1
1
Kd = 25 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0768166
 Compound Info 
(S)-2-(4-(1-acryloylpiperidin-4-yl)phenyl)-N-(5-cyclopropyl-1H-pyrazol-3-yl)propanamide
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C23H28N4O2
  1
1
Kd < 25 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0768167
 Compound Info 
(S,E)-N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-(4-(1-(4-morpholinobut-2-enoyl)-1,2,3,6-tetrahydropyridin-4-yl)phenyl)propanamide
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C28H35N5O3
  1
1
Kd < 25 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0774001
 Compound Info 
2-(4-(1-acryloyl-2,3,6,7-tetrahydro-1H-azepin-4-yl)phenyl)-N-(5-cyclopropyl-1H-pyrazol-3-yl)propanamide
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C24H28N4O2
  1
1
Kd = 25 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0833870
 Compound Info 
(S,E)-N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-(4-(1-(4-(diethylamino)but-2-enoyl)-1,2,3,6-tetrahydropyridin-4-yl)phenyl)propanamide
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C28H37N5O2
  1
1
Kd < 25 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0871647
 Compound Info 
N-(1-(4-(1-((5-cyclopropyl-1H-pyrazol-3-yl)amino)-1-oxopropan-2-yl)phenyl)piperidin-4-yl)acrylamide
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C23H29N5O2
  1
1
Kd < 25 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0912111
 Compound Info 
2-(6-(4-acryloylpiperazin-1-yl)pyridin-3-yl)-N-(5-cyclopropyl-1H-pyrazol-3-yl)propanamide
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C21H26N6O2
  1
1
Kd < 25 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0955621
 Compound Info 
(S)-2-(4-(1-acryloyl-1,2,5,6-tetrahydropyridin-3-yl)phenyl)-N-(5-cyclopropyl-1H-pyrazol-3-yl)propanamide
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C23H26N4O2
  1
1
Kd < 25 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0767889
 Compound Info 
2-(4-(1-acryloyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl)-N-(5-cyclopropyl-1H-pyrazol-3-yl)-3-methylbutanamide
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C25H30N4O2
  1
1
Kd > 100 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0871646
 Compound Info 
2-(1'-acryloyl-1',2',3',6'-tetrahydro-[2,4'-bipyridin]-5-yl)-N-(5-cyclopropyl-1H-pyrazol-3-yl)-3-methylbutanamide
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C24H29N5O2
  1
1
Kd > 100 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0702758
 Compound Info 
2-(6-(1-acryloylpiperidin-4-yl)pyridin-3-yl)-N-(5-cyclopropyl-1H-pyrazol-3-yl)propanamide
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C22H27N5O2
  1
1 IC50 = 58 nM
CP0768164
 Compound Info 
(S)-2-(4-(1-acryloyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl)-N-(5-cyclopropyl-1H-pyrazol-3-yl)propanamide
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C23H26N4O2
  1
1 IC50 = 60 nM
CP0767888
 Compound Info 
2-(4-(1-acryloyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl)-N-(5-cyclopropyl-1H-pyrazol-3-yl)propanamide
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C23H26N4O2
  1
1 IC50 = 84 nM
CP0912111
 Compound Info 
2-(6-(4-acryloylpiperazin-1-yl)pyridin-3-yl)-N-(5-cyclopropyl-1H-pyrazol-3-yl)propanamide
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C21H26N6O2
  1
1 IC50 = 99 nM
CP0768166
 Compound Info 
(S)-2-(4-(1-acryloylpiperidin-4-yl)phenyl)-N-(5-cyclopropyl-1H-pyrazol-3-yl)propanamide
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C23H28N4O2
  1
1 IC50 = 151 nM
CP0955621
 Compound Info 
(S)-2-(4-(1-acryloyl-1,2,5,6-tetrahydropyridin-3-yl)phenyl)-N-(5-cyclopropyl-1H-pyrazol-3-yl)propanamide
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C23H26N4O2
  1
1 IC50 = 189 nM
CP0702760
 Compound Info 
(S,E)-N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-(4-(1-(4-(dimethylamino)but-2-enoyl)-1,2,3,6-tetrahydropyridin-4-yl)phenyl)propanamide
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C26H33N5O2
  1
1 IC50 = 235 nM
CP0871647
 Compound Info 
N-(1-(4-(1-((5-cyclopropyl-1H-pyrazol-3-yl)amino)-1-oxopropan-2-yl)phenyl)piperidin-4-yl)acrylamide
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C23H29N5O2
  1
1 IC50 = 235 nM
CP0774001
 Compound Info 
2-(4-(1-acryloyl-2,3,6,7-tetrahydro-1H-azepin-4-yl)phenyl)-N-(5-cyclopropyl-1H-pyrazol-3-yl)propanamide
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C24H28N4O2
  1
1 IC50 = 240 nM
CP0768165
 Compound Info 
N-(4'-(1-((5-cyclopropyl-1H-pyrazol-3-yl)amino)-1-oxopropan-2-yl)-2,3,4,5-tetrahydro-[1,1-biphenyl]-4-yl)acrylamide
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C24H28N4O2
  1
1 IC50 = 380 nM
CP0768167
 Compound Info 
(S,E)-N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-(4-(1-(4-morpholinobut-2-enoyl)-1,2,3,6-tetrahydropyridin-4-yl)phenyl)propanamide
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C28H35N5O3
  1
1 IC50 = 646 nM
CP0833870
 Compound Info 
(S,E)-N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-(4-(1-(4-(diethylamino)but-2-enoyl)-1,2,3,6-tetrahydropyridin-4-yl)phenyl)propanamide
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C28H37N5O2
  1
1 IC50 = 895 nM
Clinical Information about the Protein
Target 1 ( Cyclin-dependent kinase 12 (CDK12) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Investigative Drug(s) 1 Investigative Drug  1
1 THZ531
 Drug Info 
Investigative
Solid tumour/cancer