General Information of the Protein
Protein ID
PT04100
Protein Name
Neurogenic locus notch homolog protein 1
Secondarily
Protein Name
Translocation-associated notch protein TAN-1
Gene Name
NOTCH1
Secondarily
Gene Name
TAN1
Sequence
MPPLLAPLLCLALLPALAARGPRCSQPGETCLNGGKCEAANGTEACVCGGAFVGPRCQDPNPCLSTPCKNAGTCHVVDRRGVADYACSCALGFSGPLCLTPLDNACLTNPCRNGGTCDLLTLTEYKCRCPPGWSGKSCQQADPCASNPCANGGQCLPFEASYICHCPPSFHGPTCRQDVNECGQKPGLCRHGGTCHNEVGSYRCVCRATHTGPNCERPYVPCSPSPCQNGGTCRPTGDVTHECACLPGFTGQNCEENIDDCPGNNCKNGGACVDGVNTYNCRCPPEWTGQYCTEDVDECQLMPNACQNGGTCHNTHGGYNCVCVNGWTGEDCSENIDDCASAACFHGATCHDRVASFYCECPHGRTGLLCHLNDACISNPCNEGSNCDTNPVNGKAICTCPSGYTGPACSQDVDECSLGANPCEHAGKCINTLGSFECQCLQGYTGPRCEIDVNECVSNPCQNDATCLDQIGEFQCICMPGYEGVHCEVNTDECASSPCLHNGRCLDKINEFQCECPTGFTGHLCQYDVDECASTPCKNGAKCLDGPNTYTCVCTEGYTGTHCEVDIDECDPDPCHYGSCKDGVATFTCLCRPGYTGHHCETNINECSSQPCRHGGTCQDRDNAYLCFCLKGTTGPNCEINLDDCASSPCDSGTCLDKIDGYECACEPGYTGSMCNINIDECAGNPCHNGGTCEDGINGFTCRCPEGYHDPTCLSEVNECNSNPCVHGACRDSLNGYKCDCDPGWSGTNCDINNNECESNPCVNGGTCKDMTSGYVCTCREGFSGPNCQTNINECASNPCLNQGTCIDDVAGYKCNCLLPYTGATCEVVLAPCAPSPCRNGGECRQSEDYESFSCVCPTGWQGQTCEVDINECVLSPCRHGASCQNTHGGYRCHCQAGYSGRNCETDIDDCRPNPCHNGGSCTDGINTAFCDCLPGFRGTFCEEDINECASDPCRNGANCTDCVDSYTCTCPAGFSGIHCENNTPDCTESSCFNGGTCVDGINSFTCLCPPGFTGSYCQHDVNECDSQPCLHGGTCQDGCGSYRCTCPQGYTGPNCQNLVHWCDSSPCKNGGKCWQTHTQYRCECPSGWTGLYCDVPSVSCEVAAQRQGVDVARLCQHGGLCVDAGNTHHCRCQAGYTGSYCEDLVDECSPSPCQNGATCTDYLGGYSCKCVAGYHGVNCSEEIDECLSHPCQNGGTCLDLPNTYKCSCPRGTQGVHCEINVDDCNPPVDPVSRSPKCFNNGTCVDQVGGYSCTCPPGFVGERCEGDVNECLSNPCDARGTQNCVQRVNDFHCECRAGHTGRRCESVINGCKGKPCKNGGTCAVASNTARGFICKCPAGFEGATCENDARTCGSLRCLNGGTCISGPRSPTCLCLGPFTGPECQFPASSPCLGGNPCYNQGTCEPTSESPFYRCLCPAKFNGLLCHILDYSFGGGAGRDIPPPLIEEACELPECQEDAGNKVCSLQCNNHACGWDGGDCSLNFNDPWKNCTQSLQCWKYFSDGHCDSQCNSAGCLFDGFDCQRAEGQCNPLYDQYCKDHFSDGHCDQGCNSAECEWDGLDCAEHVPERLAAGTLVVVVLMPPEQLRNSSFHFLRELSRVLHTNVVFKRDAHGQQMIFPYYGREEELRKHPIKRAAEGWAAPDALLGQVKASLLPGGSEGGRRRRELDPMDVRGSIVYLEIDNRQCVQASSQCFQSATDVAAFLGALASLGSLNIPYKIEAVQSETVEPPPPAQLHFMYVAAAAFVLLFFVGCGVLLSRKRRRQHGQLWFPEGFKVSEASKKKRREPLGEDSVGLKPLKNASDGALMDDNQNEWGDEDLETKKFRFEEPVVLPDLDDQTDHRQWTQQHLDAADLRMSAMAPTPPQGEVDADCMDVNVRGPDGFTPLMIASCSGGGLETGNSEEEEDAPAVISDFIYQGASLHNQTDRTGETALHLAARYSRSDAAKRLLEASADANIQDNMGRTPLHAAVSADAQGVFQILIRNRATDLDARMHDGTTPLILAARLAVEGMLEDLINSHADVNAVDDLGKSALHWAAAVNNVDAAVVLLKNGANKDMQNNREETPLFLAAREGSYETAKVLLDHFANRDITDHMDRLPRDIAQERMHHDIVRLLDEYNLVRSPQLHGAPLGGTPTLSPPLCSPNGYLGSLKPGVQGKKVRKPSSKGLACGSKEAKDLKARRKKSQDGKGCLLDSSGMLSPVDSLESPHGYLSDVASPPLLPSPFQQSPSVPLNHLPGMPDTHLGIGHLNVAAKPEMAALGGGGRLAFETGPPRLSHLPVASGTSTVLGSSSGGALNFTVGGSTSLNGQCEWLSRLQSGMVPNQYNPLRGSVAPGPLSTQAPSLQHGMVGPLHSSLAASALSQMMSYQGLPSTRLATQPHLVQTQQVQPQNLQMQQQNLQPANIQQQQSLQPPPPPPQPHLGVSSAASGHLGRSFLSGEPSQADVQPLGPSSLAVHTILPQESPALPTSLPSSLVPPVTAAQFLTPPSQHSYSSPVDNTPSHQLQVPEHPFLTPSPESPDQWSSSSPHSNVSDWSEGVSSPPTSMQSQIARIPEAFK
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
Function
Functions as a receptor for membrane-bound ligands Jagged-1 (JAG1), Jagged-2 (JAG2) and Delta-1 (DLL1) to regulate cell-fate determination. Upon ligand activation through the released notch intracellular domain (NICD) it forms a transcriptional activator complex with RBPJ/RBPSUH and activates genes of the enhancer of split locus. Affects the implementation of differentiation, proliferation and apoptotic programs. Involved in angiogenesis; negatively regulates endothelial cell proliferation and migration and angiogenic sprouting. Involved in the maturation of both CD4(+) and CD8(+) cells in the thymus. Important for follicular differentiation and possibly cell fate selection within the follicle. During cerebellar development, functions as a receptor for neuronal DNER and is involved in the differentiation of Bergmann glia. Represses neuronal and myogenic differentiation. May play an essential role in postimplantation development, probably in some aspect of cell specification and/or differentiation. May be involved in mesoderm development, somite formation and neurogenesis. May enhance HIF1A function by sequestering HIF1AN away from HIF1A. Required for the THBS4 function in regulating protective astrogenesis from the subventricular zone (SVZ) niche after injury. Involved in determination of left/right symmetry by modulating the balance between motile and immotile (sensory) cilia at the left-right organiser (LRO).
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Uniprot ID
Primary ID:
P46531

Secondarily ID:
Q59ED8
Q5SXM3
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Ensembl ID
ENSG00000148400
HGNC ID
HGNC:7881
Subcellular Location
Cell membrane
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: CL000017 , HeLa
Compound ID Compound Name Compound Formula
CP0409974
(2R,3R)-N'-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-2-[3-(trifluoromethyl)phenyl]-3-(3,3,3-trifluoropropyl)butanediamide
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C30H26F6N4O3
 1
1
IC50 = 1 nM
   TI
   LI
   LO
   TS
CP0410890
(2R,3R)-2-(2,4-difluorophenyl)-N'-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-3-(3,3,3-trifluoropropyl)butanediamide
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C29H25F5N4O3
 1
1
IC50 = 1 nM
   TI
   LI
   LO
   TS
CP0476835
(2S,3R)-N'-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-2-pentan-3-yl-3-(3,3,3-trifluoropropyl)butanediamide
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C28H33F3N4O3
 1
1
IC50 = 1 nM
   TI
   LI
   LO
   TS
CP0529363
US9427442, 10
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C28H28ClF5N4O3
 1
1
IC50 = 1.7 nM
   TI
   LI
   LO
   TS
CP0399659
(2R,3R)-2-(4-fluorophenyl)-N'-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-3-(3,3,3-trifluoropropyl)butanediamide
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C29H26F4N4O3
 1
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
CP0409975
(2R,3R)-2-(3,5-difluorophenyl)-N'-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-3-(3,3,3-trifluoropropyl)butanediamide
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C29H25F5N4O3
 1
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
CP0476836
(2S,3R)-N'-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-3-(2-methylpropyl)-2-pentan-3-ylbutanediamide
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C29H38N4O3
 1
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
CP0566534
(2R,3R)-2-(3,4-difluorophenyl)-N'-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-3-(3,3,3-trifluoropropyl)butanediamide
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C29H25F5N4O3
 1
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
CP0561236
US9427442, 11
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C28H28F6N4O3
 1
1
IC50 = 2.1 nM
   TI
   LI
   LO
   TS
CP0519679
US9427442, 18
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C25H25F5N4O3
 1
1
IC50 = 2.7 nM
   TI
   LI
   LO
   TS
CP0561238
US9427442, 13
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C27H26ClF5N4O3
 1
1
IC50 = 2.8 nM
   TI
   LI
   LO
   TS
CP0518667
US9427442, 8
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C28H29F5N4O4
 1
1
IC50 = 2.9 nM
   TI
   LI
   LO
   TS
CP0561154
US9427442, 19
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C26H25F7N4O3
 1
1
IC50 = 2.9 nM
   TI
   LI
   LO
   TS
CP0399658
(2S,3R)-3-(2,2-dimethylpropyl)-N'-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-2-pentan-3-ylbutanediamide
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C30H40N4O3
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0410889
(2R,3R)-2-(3-methyl-1,2-oxazol-4-yl)-N'-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-3-(3,3,3-trifluoropropyl)butanediamide
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C27H26F3N5O4
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0428750
(2R,3R)-N'-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-2-[3-(trifluoromethoxy)phenyl]-3-(3,3,3-trifluoropropyl)butanediamide
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C30H26F6N4O4
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0542514
(2R,3R)-N'-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-2-(3-methylphenyl)-3-(3,3,3-trifluoropropyl)butanediamide
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C30H29F3N4O3
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0556713
US9427442, 1
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C28H29F5N4O3
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0486300
US9427442, 22
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C26H25ClF6N4O3
 1
1
IC50 = 3.2 nM
   TI
   LI
   LO
   TS
CP0539483
US9427442, 9
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C28H28F6N4O3
 1
1
IC50 = 3.5 nM
   TI
   LI
   LO
   TS
CP0419410
US9427442, 25
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C28H30F4N4O3
 1
1
IC50 = 3.8 nM
   TI
   LI
   LO
   TS
CP0539484
US9427442, 24
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C26H26ClF5N4O3
 1
1
IC50 = 3.9 nM
   TI
   LI
   LO
   TS
CP0552247
US9427442, 7
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C30H31F5N4O4
 1
1
IC50 = 3.9 nM
   TI
   LI
   LO
   TS
CP0486923
(2R,3R)-N'-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-2-phenyl-3-(3,3,3-trifluoropropyl)butanediamide
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C29H27F3N4O3
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0402631
US9427442, 3
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C31H32F6N4O4
 1
1
IC50 = 4.2 nM
   TI
   LI
   LO
   TS
CP0419462
US9427442, 15
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C27H27F5N4O3
 1
1
IC50 = 4.4 nM
   TI
   LI
   LO
   TS
CP0419464
US9427442, 5
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C28H28ClF5N4O3
 1
1
IC50 = 4.4 nM
   TI
   LI
   LO
   TS
CP0402632
US9427442, 14
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C27H26F6N4O3
 1
1
IC50 = 4.5 nM
   TI
   LI
   LO
   TS
CP0412022
US9273014, Comparative Compound 47
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C28H35ClN4O3
 1
1
IC50 = 5.1 nM
   TI
   LI
   LO
   TS
CP0515744
US9427442, 23
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C26H25ClF6N4O3
 1
1
IC50 = 5.1 nM
   TI
   LI
   LO
   TS
CP0556307
US9427442, 12
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C30H31F5N4O3
 1
1
IC50 = 5.6 nM
   TI
   LI
   LO
   TS
CP0466215
US9427442, 17
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C26H28F4N4O4
 1
1
IC50 = 5.8 nM
   TI
   LI
   LO
   TS
CP0561153
US9427442, 16
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C25H27F4N5O4
 1
1
IC50 = 7 nM
   TI
   LI
   LO
   TS
CP0561237
US9427442, 2
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C29H31F5N4O4
 1
1
IC50 = 7 nM
   TI
   LI
   LO
   TS
CP0553703
US9427442, 21
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C27H29F5N4O4
 1
1
IC50 = 7.5 nM
   TI
   LI
   LO
   TS
CP0471072
(2R,3R)-2-(4-methoxyphenyl)-N'-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-3-(3,3,3-trifluoropropyl)butanediamide
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C30H29F3N4O4
 1
1
IC50 = 9 nM
   TI
   LI
   LO
   TS
CP0486299
US9427442, 20
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C25H25ClF4N4O3
 1
1
IC50 = 10.8 nM
   TI
   LI
   LO
   TS
CP0537195
US9427442, 4
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C29H29ClF6N4O3
 1
1
IC50 = 11.9 nM
   TI
   LI
   LO
   TS
CP0428820
US9273014, Comparative Compound 48
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C29H36N4O3
 1
1
IC50 = 12.3 nM
   TI
   LI
   LO
   TS
CP0542515
(2S,3R)-N'-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-2-propyl-3-(2,2,2-trifluoroethyl)butanediamide
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C25H27F3N4O3
 1
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0561235
US9427442, 6
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C26H25F5N4O3
 1
1
IC50 = 14 nM
   TI
   LI
   LO
   TS
CP0472376
(2R,3R)-2-(1,2-oxazol-4-yl)-N'-[(3S)-2-oxo-5-phenyl-1,3-dihydro-1,4-benzodiazepin-3-yl]-3-(3,3,3-trifluoropropyl)butanediamide
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C25H22F3N5O4
 1
1
IC50 = 32 nM
   TI
   LI
   LO
   TS
CP0491589
US9273014, Comparative Compound 46
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C27H31ClN4O3
 1
1
IC50 = 42.4 nM
   TI
   LI
   LO
   TS
CP0481233
(2R,3R)-2-(5-methyl-1,2-oxazol-3-yl)-N'-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-3-(3,3,3-trifluoropropyl)butanediamide
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C27H26F3N5O4
 1
1
IC50 = 54 nM
   TI
   LI
   LO
   TS
CP0004510
US9273014, Comparative Compound 45
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C27H34N4O3
 1
1
IC50 = 64.1 nM
   TI
   LI
   LO
   TS
CP0400691
(2R,3R)-2-(5-methyl-1,2,4-oxadiazol-3-yl)-N'-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-3-(3,3,3-trifluoropropyl)butanediamide
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C26H25F3N6O4
 1
1
IC50 = 169 nM
   TI
   LI
   LO
   TS
CP0399657
(2R,3R)-2-(1,3-oxazol-4-yl)-N'-[(3S)-2-oxo-5-phenyl-1,3-dihydro-1,4-benzodiazepin-3-yl]-3-(3,3,3-trifluoropropyl)butanediamide
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C25H22F3N5O4
 1
1
IC50 = 231 nM
   TI
   LI
   LO
   TS
CP0381969
(2R,3R)-2-(1,2,4-oxadiazol-3-yl)-N'-[(3S)-2-oxo-5-phenyl-1,3-dihydro-1,4-benzodiazepin-3-yl]-3-(3,3,3-trifluoropropyl)butanediamide
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C24H21F3N6O4
 1
1
IC50 = 1190 nM
   TI
   LI
   LO
   TS
CP0480596
(2R,3R)-N'-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-2-(3-methylsulfonylphenyl)-3-(3,3,3-trifluoropropyl)butanediamide
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C30H29F3N4O5S
 1
1
IC50 = 2060 nM
   TI
   LI
   LO
   TS
Clinical Information about the Protein
Target 1 ( Notch-1 receptor (NOTCH1) )
Target Type Clinical trial Target
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT06342 Neurogenic locus notch homolog protein 1 Mus musculus, Mouse