Reaction Details |
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Target | cAMP-dependent protein kinase catalytic subunit alpha/beta/gamma |
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Ligand | BDBM50204693 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_442106 (CHEMBL891244) |
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IC50 | >50000±n/a nM |
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Citation | Tong, Y; Claiborne, A; Stewart, KD; Park, C; Kovar, P; Chen, Z; Credo, RB; Gu, WZ; Gwaltney, SL; Judge, RA; Zhang, H; Rosenberg, SH; Sham, HL; Sowin, TJ; Lin, NH Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors. Bioorg Med Chem15:2759-67 (2007) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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cAMP-dependent protein kinase catalytic subunit alpha/beta/gamma |
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Name: | cAMP-dependent protein kinase catalytic subunit alpha/beta/gamma |
Synonyms: | cAMP-dependent protein kinase (PKA) |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of ChEMBL is 217489 |
Components: | This complex has 3 components. |
Component 1 |
Name: | cAMP-dependent protein kinase catalytic subunit beta |
Synonyms: | KAPCB_HUMAN | PKA C-beta | PKAC-beta | PRKACB | cAMP-dependent protein kinase (PKA) | cAMP-dependent protein kinase beta-1 catalytic subunit | cAMP-dependent protein kinase catalytic subunit beta |
Type: | PROTEIN |
Mol. Mass.: | 40631.25 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_586348 |
Residue: | 351 |
Sequence: | MGNAATAKKGSEVESVKEFLAKAKEDFLKKWENPTQNNAGLEDFERKKTLGTGSFGRVML
VKHKATEQYYAMKILDKQKVVKLKQIEHTLNEKRILQAVNFPFLVRLEYAFKDNSNLYMV
MEYVPGGEMFSHLRRIGRFSEPHARFYAAQIVLTFEYLHSLDLIYRDLKPENLLIDHQGY
IQVTDFGFAKRVKGRTWTLCGTPEYLAPEIILSKGYNKAVDWWALGVLIYEMAAGYPPFF
ADQPIQIYEKIVSGKVRFPSHFSSDLKDLLRNLLQVDLTKRFGNLKNGVSDIKTHKWFAT
TDWIAIYQRKVEAPFIPKFRGSGDTSNFDDYEEEDIRVSITEKCAKEFGEF
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Component 2 |
Name: | cAMP-dependent protein kinase catalytic subunit alpha |
Synonyms: | KAPCA_HUMAN | PKA C-alpha | PKACA | PRKACA | cAMP-dependent protein kinase (PKA) | cAMP-dependent protein kinase catalytic (PKA) | cAMP-dependent protein kinase catalytic subunit alpha | cAMP-dependent protein kinase catalytic subunit alpha (PKA) | cAMP-dependent protein kinase catalytic subunit alpha (PKACA) | cAMP-dependent protein kinase catalytic subunit alpha (PKAc) | cAMP-dependent protein kinase catalytic subunit alpha isoform 1 | cAMP-dependent protein kinase, alpha-catalytic subunit |
Type: | Enzyme Catalytic Subunit |
Mol. Mass.: | 40598.73 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 351 |
Sequence: | MGNAAAAKKGSEQESVKEFLAKAKEDFLKKWESPAQNTAHLDQFERIKTLGTGSFGRVML
VKHKETGNHYAMKILDKQKVVKLKQIEHTLNEKRILQAVNFPFLVKLEFSFKDNSNLYMV
MEYVPGGEMFSHLRRIGRFSEPHARFYAAQIVLTFEYLHSLDLIYRDLKPENLLIDQQGY
IQVTDFGFAKRVKGRTWTLCGTPEYLAPEIILSKGYNKAVDWWALGVLIYEMAAGYPPFF
ADQPIQIYEKIVSGKVRFPSHFSSDLKDLLRNLLQVDLTKRFGNLKNGVNDIKNHKWFAT
TDWIAIYQRKVEAPFIPKFKGPGDTSNFDDYEEEEIRVSINEKCGKEFSEF
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Component 3 |
Name: | cAMP-dependent protein kinase catalytic subunit gamma |
Synonyms: | KAPCG_HUMAN | PKA C-gamma | PRKACG | cAMP-dependent protein kinase (PKA) | cAMP-dependent protein kinase catalytic subunit gamma |
Type: | PROTEIN |
Mol. Mass.: | 40442.03 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_104720 |
Residue: | 351 |
Sequence: | MGNAPAKKDTEQEESVNEFLAKARGDFLYRWGNPAQNTASSDQFERLRTLGMGSFGRVML
VRHQETGGHYAMKILNKQKVVKMKQVEHILNEKRILQAIDFPFLVKLQFSFKDNSYLYLV
MEYVPGGEMFSRLQRVGRFSEPHACFYAAQVVLAVQYLHSLDLIHRDLKPENLLIDQQGY
LQVTDFGFAKRVKGRTWTLCGTPEYLAPEIILSKGYNKAVDWWALGVLIYEMAVGFPPFY
ADQPIQIYEKIVSGRVRFPSKLSSDLKHLLRSLLQVDLTKRFGNLRNGVGDIKNHKWFAT
TSWIAIYEKKVEAPFIPKYTGPGDASNFDDYEEEELRISINEKCAKEFSEF
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BDBM50204693 |
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n/a |
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Name | BDBM50204693 |
Synonyms: | 3-(4'-hydroxy-biphenyl-4-yl)-1,4-dihydro-indeno[1,2-c]pyrazole-6-carboxylic acid (pyridin-4-ylmethyl)-amide | CHEMBL242753 |
Type | Small organic molecule |
Emp. Form. | C29H22N4O2 |
Mol. Mass. | 458.5106 |
SMILES | Oc1ccc(cc1)-c1ccc(cc1)-c1n[nH]c-2c1Cc1cc(ccc-21)C(=O)NCc1ccncc1 |
Structure |
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