General Information of the Protein
Protein ID
PT03759
Protein Name
NPC intracellular cholesterol transporter 1
Secondarily
Protein Name
Niemann-Pick C1 protein
Gene Name
NPC1
Sequence
MTARGLALGLLLLLLCPAQVFSQSCVWYGECGIAYGDKRYNCEYSGPPKPLPKDGYDLVQELCPGFFFGNVSLCCDVRQLQTLKDNLQLPLQFLSRCPSCFYNLLNLFCELTCSPRQSQFLNVTATEDYVDPVTNQTKTNVKELQYYVGQSFANAMYNACRDVEAPSSNDKALGLLCGKDADACNATNWIEYMFNKDNGQAPFTITPVFSDFPVHGMEPMNNATKGCDESVDEVTAPCSCQDCSIVCGPKPQPPPPPAPWTILGLDAMYVIMWITYMAFLLVFFGAFFAVWCYRKRYFVSEYTPIDSNIAFSVNASDKGEASCCDPVSAAFEGCLRRLFTRWGSFCVRNPGCVIFFSLVFITACSSGLVFVRVTTNPVDLWSAPSSQARLEKEYFDQHFGPFFRTEQLIIRAPLTDKHIYQPYPSGADVPFGPPLDIQILHQVLDLQIAIENITASYDNETVTLQDICLAPLSPYNTNCTILSVLNYFQNSHSVLDHKKGDDFFVYADYHTHFLYCVRAPASLNDTSLLHDPCLGTFGGPVFPWLVLGGYDDQNYNNATALVITFPVNNYYNDTEKLQRAQAWEKEFINFVKNYKNPNLTISFTAERSIEDELNRESDSDVFTVVISYAIMFLYISLALGHMKSCRRLLVDSKVSLGIAGILIVLSSVACSLGVFSYIGLPLTLIVIEVIPFLVLAVGVDNIFILVQAYQRDERLQGETLDQQLGRVLGEVAPSMFLSSFSETVAFFLGALSVMPAVHTFSLFAGLAVFIDFLLQITCFVSLLGLDIKRQEKNRLDIFCCVRGAEDGTSVQASESCLFRFFKNSYSPLLLKDWMRPIVIAIFVGVLSFSIAVLNKVDIGLDQSLSMPDDSYMVDYFKSISQYLHAGPPVYFVLEEGHDYTSSKGQNMVCGGMGCNNDSLVQQIFNAAQLDNYTRIGFAPSSWIDDYFDWVKPQSSCCRVDNITDQFCNASVVDPACVRCRPLTPEGKQRPQGGDFMRFLPMFLSDNPNPKCGKGGHAAYSSAVNILLGHGTRVGATYFMTYHTVLQTSADFIDALKKARLIASNVTETMGINGSAYRVFPYSVFYVFYEQYLTIIDDTIFNLGVSLGAIFLVTMVLLGCELWSAVIMCATIAMVLVNMFGVMWLWGISLNAVSLVNLVMSCGISVEFCSHITRAFTVSMKGSRVERAEEALAHMGSSVFSGITLTKFGGIVVLAFAKSQIFQIFYFRMYLAMVLLGATHGLIFLPVLLSYIGPSVNKAKSCATEERYKGTERERLLNF
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Organism
Homo sapiens, Human
Protein Classification
Transporter
Function
Intracellular cholesterol transporter which acts in concert with NPC2 and plays an important role in the egress of cholesterol from the endosomal/lysosomal compartment (PubMed:9211849, PubMed:9927649, PubMed:10821832, PubMed:18772377, PubMed:27238017, PubMed:12554680). Unesterified cholesterol that has been released from LDLs in the lumen of the late endosomes/lysosomes is transferred by NPC2 to the cholesterol-binding pocket in the N-terminal domain of NPC1 (PubMed:9211849, PubMed:9927649, PubMed:18772377, PubMed:19563754, PubMed:27238017, PubMed:28784760). Cholesterol binds to NPC1 with the hydroxyl group buried in the binding pocket (PubMed:19563754). Binds oxysterol with higher affinity than cholesterol. May play a role in vesicular trafficking in glia, a process that may be crucial for maintaining the structural and functional integrity of nerve terminals (Probable). Inhibits cholesterol-mediated mTORC1 activation throught its interaction with SLC38A9 (PubMed:28336668).
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Uniprot ID
Primary ID:
O15118

Secondarily ID:
B4DET3
Q9P130
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Ensembl ID
ENSG00000141458
HGNC ID
HGNC:7897
Subcellular Location
Late endosome membrane
Lysosome 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: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0481959
2-[[(3S,5R,6R,8S,9S,10R,13R,14S,17R)-5,6-dihydroxy-10,13-dimethyl-17-[(2R)-6-methylheptan-2-yl]-1,2,3,4,6,7,8,9,11,12,14,15,16,17-tetradecahydrocyclopenta[a]phenanthren-3-yl]oxy]-1-morpholin-4-ylethanone
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C33H57NO5
 1
1
EC50 = 150 nM
   TI
   LI
   LO
   TS
CP0538986
5-(cyclohexylmethyl)-6-oxophenanthridine-2-carboxamide
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C21H22N2O2
 1
1
EC50 = 3600 nM
   TI
   LI
   LO
   TS
CP0567149
6-oxo-5-pentylphenanthridine-2-carboxamide
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C19H20N2O2
 1
1
EC50 = 4200 nM
   TI
   LI
   LO
   TS
CP0414298
5-butyl-6-oxophenanthridine-2-carboxamide
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C18H18N2O2
 1
1
EC50 = 11000 nM
   TI
   LI
   LO
   TS
CP0463417
5-butyl-6-oxo-8,9,10,11-tetrahydro-7H-cyclohepta[c]quinoline-2-carboxamide
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C19H24N2O2
 1
1
EC50 = 13000 nM
   TI
   LI
   LO
   TS
CP0481957
N-(5-butyl-6-oxophenanthridin-2-yl)methanesulfonamide
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C18H20N2O3S
 1
1
EC50 = 14000 nM
   TI
   LI
   LO
   TS
CP0544856
N-(5-butyl-6-oxophenanthridin-2-yl)acetamide
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C19H20N2O2
 1
1
EC50 = 14000 nM
   TI
   LI
   LO
   TS
CP0544857
6-oxo-5-(2-trimethylsilylethoxymethyl)phenanthridine-2-carboxamide
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C20H24N2O3Si
 1
1
EC50 = 16000 nM
   TI
   LI
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   TS
CP0558583
6-oxo-5-propylphenanthridine-2-carboxamide
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C17H16N2O2
 1
1
EC50 = 19000 nM
   TI
   LI
   LO
   TS
CP0414182
5-butyl-N,N-bis(2-hydroxyethyl)-6-oxophenanthridine-2-carboxamide
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C22H26N2O4
 1
1
EC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0459434
5-butyl-2-(hydroxymethyl)phenanthridin-6-one
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C18H19NO2
 1
1
EC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0463408
5-butyl-N-methyl-6-oxophenanthridine-2-carboxamide
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C19H20N2O2
 1
1
EC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0481958
5-butyl-N,N-dimethyl-6-oxophenanthridine-2-carboxamide
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C20H22N2O2
 1
1
EC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0507022
5-butyl-2-(1-hydroxyethyl)phenanthridin-6-one
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C19H21NO2
 1
1
EC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0507023
5-butyl-2-hydroxyphenanthridin-6-one
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C17H17NO2
 1
1
EC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0534204
6-oxo-5-prop-2-enylphenanthridine-2-carboxamide
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C17H14N2O2
 1
1
EC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0535861
2-acetyl-5-butylphenanthridin-6-one
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C19H19NO2
 1
1
EC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0544855
5-methyl-6-oxophenanthridine-2-carboxamide
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C15H12N2O2
 1
1
EC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0558584
5-butyl-6-oxo-7,8,9,10-tetrahydrophenanthridine-2-carboxamide
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C18H22N2O2
 1
1
EC50 = 30000 nM
   TI
   LI
   LO
   TS
CP0567150
5-ethyl-6-oxophenanthridine-2-carboxamide
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C16H14N2O2
 1
1
EC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0538987
5-heptyl-6-oxophenanthridine-2-carboxamide
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C21H24N2O2
 1
1
EC50 > 3000 nM
   TI
   LI
   LO
   TS
CP0567148
5-hexyl-6-oxophenanthridine-2-carboxamide
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C20H22N2O2
 1
1
EC50 > 3000 nM
   TI
   LI
   LO
   TS