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Target Report Card

Target Name and Classification

Target ID CHEMBL2146346
Preferred Name Neurogenic locus notch homolog protein 1
Synonyms NEXT | NICD | NOTCH1 | Neurogenic locus notch homolog protein 1 | Notch 1 extracellular truncation | Notch 1 intracellular domain | Notch 1 | TAN1 | Translocation-associated notch protein TAN-1 | hN1
Organism Homo sapiens
Species Group No
Protein Target Classification
  • unclassified protein

Target Components

Component Description Relationship Accession
Neurogenic locus notch homolog protein 1 SINGLE PROTEIN P46531

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL3545261 BRONTICTUZUMAB Neurogenic locus notch homolog protein 1 inhibitor 1 Other PubMed PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000148400
Ensembl ENSG00000148400
GO Cellular Component GO:0000139 (Golgi membrane)
GO:0001669 (acrosomal vesicle)
GO:0002193 (MAML1-RBP-Jkappa- ICN1 complex)
GO:0005576 (extracellular region)
GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0005737 (cytoplasm)
GO:0005783 (endoplasmic reticulum)
GO:0005789 (endoplasmic reticulum membrane)
GO:0005794 (Golgi apparatus)
GO:0005829 (cytosol)
GO:0005886 (plasma membrane)
GO:0005912 (adherens junction)
GO:0009986 (cell surface)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0016324 (apical plasma membrane)
GO:0031410 (cytoplasmic vesicle)
GO:0043235 (receptor complex)
GO:0071944 (cell periphery)
GO Molecular Function GO:0001047 (core promoter binding)
GO:0001190 (transcriptional activator activity, RNA polymerase II transcription factor binding)
GO:0003682 (chromatin binding)
GO:0003700 (transcription factor activity, sequence-specific DNA binding)
GO:0004857 (enzyme inhibitor activity)
GO:0004888 (transmembrane signaling receptor activity)
GO:0005112 (Notch binding)
GO:0005509 (calcium ion binding)
GO:0005515 (protein binding)
GO:0019899 (enzyme binding)
GO:0031490 (chromatin DNA binding)
GO:0038023 (signaling receptor activity)
GO:0043565 (sequence-specific DNA binding)
GO:0046872 (metal ion binding)
GO:0046982 (protein heterodimerization activity)
GO Biological Process GO:0000122 (negative regulation of transcription from RNA polymerase II promoter)
GO:0001525 (angiogenesis)
GO:0001701 (in utero embryonic development)
GO:0001708 (cell fate specification)
GO:0001837 (epithelial to mesenchymal transition)
GO:0001889 (liver development)
GO:0001947 (heart looping)
GO:0002040 (sprouting angiogenesis)
GO:0002052 (positive regulation of neuroblast proliferation)
GO:0002437 (inflammatory response to antigenic stimulus)
GO:0003157 (endocardium development)
GO:0003160 (endocardium morphogenesis)
GO:0003162 (atrioventricular node development)
GO:0003169 (coronary vein morphogenesis)
GO:0003180 (aortic valve morphogenesis)
GO:0003181 (atrioventricular valve morphogenesis)
GO:0003184 (pulmonary valve morphogenesis)
GO:0003192 (mitral valve formation)
GO:0003197 (endocardial cushion development)
GO:0003198 (epithelial to mesenchymal transition involved in endocardial cushion formation)
GO:0003203 (endocardial cushion morphogenesis)
GO:0003207 (cardiac chamber formation)
GO:0003208 (cardiac ventricle morphogenesis)
GO:0003209 (cardiac atrium morphogenesis)
GO:0003213 (cardiac right atrium morphogenesis)
GO:0003214 (cardiac left ventricle morphogenesis)
GO:0003219 (cardiac right ventricle formation)
GO:0003222 (ventricular trabecula myocardium morphogenesis)
GO:0003241 (growth involved in heart morphogenesis)
GO:0003256 (regulation of transcription from RNA polymerase II promoter involved in myocardial precursor cell differentiation)
GO:0003264 (regulation of cardioblast proliferation)
GO:0003270 (Notch signaling pathway involved in regulation of secondary heart field cardioblast proliferation)
GO:0003273 (cell migration involved in endocardial cushion formation)
GO:0003344 (pericardium morphogenesis)
GO:0006351 (transcription, DNA-templated)
GO:0006355 (regulation of transcription, DNA-templated)
GO:0006357 (regulation of transcription from RNA polymerase II promoter)
GO:0006367 (transcription initiation from RNA polymerase II promoter)
GO:0006955 (immune response)
GO:0006959 (humoral immune response)
GO:0007050 (cell cycle arrest)
GO:0007219 (Notch signaling pathway)
GO:0007221 (positive regulation of transcription of Notch receptor target)
GO:0007275 (multicellular organism development)
GO:0007283 (spermatogenesis)
GO:0007368 (determination of left/right symmetry)
GO:0007386 (compartment pattern specification)
GO:0007409 (axonogenesis)
GO:0007420 (brain development)
GO:0007440 (foregut morphogenesis)
GO:0007492 (endoderm development)
GO:0007507 (heart development)
GO:0008284 (positive regulation of cell proliferation)
GO:0008285 (negative regulation of cell proliferation)
GO:0008544 (epidermis development)
GO:0008593 (regulation of Notch signaling pathway)
GO:0009912 (auditory receptor cell fate commitment)
GO:0010001 (glial cell differentiation)
GO:0010468 (regulation of gene expression)
GO:0010629 (negative regulation of gene expression)
GO:0010718 (positive regulation of epithelial to mesenchymal transition)
GO:0010812 (negative regulation of cell-substrate adhesion)
GO:0010832 (negative regulation of myotube differentiation)
GO:0014031 (mesenchymal cell development)
GO:0014807 (regulation of somitogenesis)
GO:0021515 (cell differentiation in spinal cord)
GO:0021915 (neural tube development)
GO:0030154 (cell differentiation)
GO:0030182 (neuron differentiation)
GO:0030216 (keratinocyte differentiation)
GO:0030279 (negative regulation of ossification)
GO:0030324 (lung development)
GO:0030326 (embryonic limb morphogenesis)
GO:0030334 (regulation of cell migration)
GO:0030335 (positive regulation of cell migration)
GO:0030513 (positive regulation of BMP signaling pathway)
GO:0030514 (negative regulation of BMP signaling pathway)
GO:0030900 (forebrain development)
GO:0031069 (hair follicle morphogenesis)
GO:0031100 (organ regeneration)
GO:0031960 (response to corticosteroid)
GO:0032495 (response to muramyl dipeptide)
GO:0032496 (response to lipopolysaccharide)
GO:0035116 (embryonic hindlimb morphogenesis)
GO:0035148 (tube formation)
GO:0035914 (skeletal muscle cell differentiation)
GO:0035924 (cellular response to vascular endothelial growth factor stimulus)
GO:0042127 (regulation of cell proliferation)
GO:0042246 (tissue regeneration)
GO:0043065 (positive regulation of apoptotic process)
GO:0043086 (negative regulation of catalytic activity)
GO:0045070 (positive regulation of viral genome replication)
GO:0045165 (cell fate commitment)
GO:0045596 (negative regulation of cell differentiation)
GO:0045603 (positive regulation of endothelial cell differentiation)
GO:0045607 (regulation of auditory receptor cell differentiation)
GO:0045608 (negative regulation of auditory receptor cell differentiation)
GO:0045618 (positive regulation of keratinocyte differentiation)
GO:0045662 (negative regulation of myoblast differentiation)
GO:0045665 (negative regulation of neuron differentiation)
GO:0045668 (negative regulation of osteoblast differentiation)
GO:0045687 (positive regulation of glial cell differentiation)
GO:0045747 (positive regulation of Notch signaling pathway)
GO:0045892 (negative regulation of transcription, DNA-templated)
GO:0045893 (positive regulation of transcription, DNA-templated)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0045955 (negative regulation of calcium ion-dependent exocytosis)
GO:0045967 (negative regulation of growth rate)
GO:0046427 (positive regulation of JAK-STAT cascade)
GO:0046533 (negative regulation of photoreceptor cell differentiation)
GO:0046579 (positive regulation of Ras protein signal transduction)
GO:0048103 (somatic stem cell division)
GO:0048663 (neuron fate commitment)
GO:0048708 (astrocyte differentiation)
GO:0048709 (oligodendrocyte differentiation)
GO:0048711 (positive regulation of astrocyte differentiation)
GO:0048715 (negative regulation of oligodendrocyte differentiation)
GO:0048754 (branching morphogenesis of an epithelial tube)
GO:0048845 (venous blood vessel morphogenesis)
GO:0050678 (regulation of epithelial cell proliferation)
GO:0050679 (positive regulation of epithelial cell proliferation)
GO:0050767 (regulation of neurogenesis)
GO:0050768 (negative regulation of neurogenesis)
GO:0050793 (regulation of developmental process)
GO:0055008 (cardiac muscle tissue morphogenesis)
GO:0060038 (cardiac muscle cell proliferation)
GO:0060045 (positive regulation of cardiac muscle cell proliferation)
GO:0060253 (negative regulation of glial cell proliferation)
GO:0060271 (cilium morphogenesis)
GO:0060317 (cardiac epithelial to mesenchymal transition)
GO:0060411 (cardiac septum morphogenesis)
GO:0060412 (ventricular septum morphogenesis)
GO:0060528 (secretory columnal luminar epithelial cell differentiation involved in prostate glandular acinus development)
GO:0060548 (negative regulation of cell death)
GO:0060740 (prostate gland epithelium morphogenesis)
GO:0060768 (regulation of epithelial cell proliferation involved in prostate gland development)
GO:0060842 (arterial endothelial cell differentiation)
GO:0060843 (venous endothelial cell differentiation)
GO:0060948 (cardiac vascular smooth muscle cell development)
GO:0060956 (endocardial cell differentiation)
GO:0060979 (vasculogenesis involved in coronary vascular morphogenesis)
GO:0060982 (coronary artery morphogenesis)
GO:0061314 (Notch signaling involved in heart development)
GO:0061384 (heart trabecula morphogenesis)
GO:0061419 (positive regulation of transcription from RNA polymerase II promoter in response to hypoxia)
GO:0070374 (positive regulation of ERK1 and ERK2 cascade)
GO:0070986 (left/right axis specification)
GO:0071372 (cellular response to follicle-stimulating hormone stimulus)
GO:0072017 (distal tubule development)
GO:0072044 (collecting duct development)
GO:0072144 (glomerular mesangial cell development)
GO:0072602 (interleukin-4 secretion)
GO:0090051 (negative regulation of cell migration involved in sprouting angiogenesis)
GO:0090090 (negative regulation of canonical Wnt signaling pathway)
GO:0097150 (neuronal stem cell population maintenance)
GO:1901201 (regulation of extracellular matrix assembly)
GO:1902263 (apoptotic process involved in embryonic digit morphogenesis)
GO:1903849 (positive regulation of aorta morphogenesis)
GO:2000737 (negative regulation of stem cell differentiation)
GO:2000811 (negative regulation of anoikis)
GO:2000974 (negative regulation of pro-B cell differentiation)
GO:2001027 (negative regulation of endothelial cell chemotaxis)

Target Cross References - Protein

CGD Aortic valve disease
Human Protein Atlas ENSG00000148400
IntAct P46531
Open Targets ENSG00000148400
PharmGKB PA31683
Reactome R-HSA-1912399 (Pre-NOTCH Processing in the Endoplasmic Reticulum.)
R-HSA-1912408 (Pre-NOTCH Transcription and Translation.)
R-HSA-1912420 (Pre-NOTCH Processing in Golgi.)
R-HSA-210744 (Regulation of gene expression in late stage (branching morphogenesis) pancreatic bud precursor cells.)
R-HSA-2122947 (NOTCH1 Intracellular Domain Regulates Transcription.)
R-HSA-2122948 (Activated NOTCH1 Transmits Signal to the Nucleus.)
R-HSA-2644606 (Constitutive Signaling by NOTCH1 PEST Domain Mutants.)
R-HSA-2644607 (Loss of Function of FBXW7 in Cancer and NOTCH1 Signaling.)
R-HSA-2660826 (Constitutive Signaling by NOTCH1 t(7;9)(NOTCH1:M1580_K2555) Translocation Mutant.)
R-HSA-2691232 (Constitutive Signaling by NOTCH1 HD Domain Mutants.)
R-HSA-2894862 (Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants.)
R-HSA-350054 (Notch-HLH transcription pathway.)
R-HSA-5083630 (Defective LFNG causes SCDO3.)
R-HSA-8941856 (RUNX3 regulates NOTCH signaling.)
R-HSA-9013508 (NOTCH3 Intracellular Domain Regulates Transcription.)
UniProt P46531 Q59ED8 Q5SXM3

Target Cross References - Domain

InterPro IPR000152 (EGF-type_Asp/Asn_hydroxyl_site.)
IPR000742 (EGF-like_dom.)
IPR000800 (Notch_dom.)
IPR001881 (EGF-like_Ca-bd_dom.)
IPR002110 (Ankyrin_rpt.)
IPR008297 (Notch.)
IPR009030 (Growth_fac_rcpt_cys_sf.)
IPR010660 (Notch_NOD_dom.)
IPR011656 (Notch_NODP_dom.)
IPR013032 (EGF-like_CS.)
IPR018097 (EGF_Ca-bd_CS.)
IPR020683 (Ankyrin_rpt-contain_dom.)
IPR022362 (Notch_1.)
IPR024600 (DUF3454_notch.)
IPR035993 (Notch-like_dom_sf.)
IPR036770 (Ankyrin_rpt-contain_sf.)
Pfam PF00008 (EGF)
PF00066 (Notch)
PF06816 (NOD)
PF07645 (EGF_CA)
PF07684 (NODP)
PF11936 (DUF3454)
PF12661 (hEGF)
PF12796 (Ank_2)

Target Cross References - Structure

PDBe 1YYH 2F8X 2F8Y 2HE0 2VJ3 3ETO 3I08 3L95 3NBN 3V79 4CUD 4CUE 4CUF 4D0E 4D0F 5FM9 5FMA 5L0R 5UB5
CREDO 1YYH 2F8X 2F8Y 2HE0 2VJ3 3ETO 3I08 3L95 3NBN 3V79 4CUD 4CUE 4CUF 4D0E 4D0F 5FM9 5FMA 5L0R 5UB5