General Information of the Protein
Protein ID
PT02397
Protein Name
Protein smoothened
Gene Name
SMO
Secondarily
Gene Name
Smoh
Sequence
MAAGRPVRGPELAPRRLLQLLLLVLLGGPGRGAALSGNVTGPGPHSASGSSRRDVPVTSPPPPLLSHCGRAAHCEPLRYNVCLGSALPYGATTTLLAGDSDSQEEAHGKLVLWSGLRNAPRCWAVIQPLLCAVYMPKCENDRVELPSRTLCQATRGPCAIVERERGWPDFLRCTPDHFPEGCPNEVQNIKFNSSGQCEAPLVRTDNPKSWYEDVEGCGIQCQNPLFTEAEHQDMHSYIAAFGAVTGLCTLFTLATFVADWRNSNRYPAVILFYVNACFFVGSIGWLAQFMDGARREIVCRADGTMRFGEPTSSETLSCVIIFVIVYYALMAGVVWFVVLTYAWHTSFKALGTTYQPLSGKTSYFHLLTWSLPFVLTVAILAVAQVDGDSVSGICFVGYKNYRYRAGFVLAPIGLVLIVGGYFLIRGVMTLFSIKSNHPGLLSEKAASKINETMLRLGIFGFLAFGFVLITFSCHFYDFFNQAEWERSFRDYVLCQANVTIGLPTKKPIPDCEIKNRPSLLVEKINLFAMFGTGIAMSTWVWTKATLLIWRRTWCRLTGHSDDEPKRIKKSKMIAKAFSKRRELLQNPGQELSFSMHTVSHDGPVAGLAFDLNEPSADVSSAWAQHVTKMVARRGAILPQDVSVTPVATPVPPEEQANMWLVEAEISPELEKRLGRKKKRRKRKKEVCPLRPAPELHHSAPVPATSAVPRLPQLPRQKCLVAANAWGTGESCRQGAWTLVSNPFCPEPSPHQDPFLPGASAPRVWAQGRLQGLGSIHSRTNLMEAEILDADSDF
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Organism
Mus musculus, Mouse
Protein Classification
Membrane receptor
>
Frizzled family G protein-coupled receptor
>
Smoothened receptor (frizzled family GPCR)
Function
G protein-coupled receptor which associates with the patched protein (PTCH) to transduce hedgehog protein signaling. Binding of sonic hedgehog (SHH) to its receptor patched prevents inhibition of smoothened (SMO) by patched (By similarity). When active, SMO binds to and sequesters protein kinase A catalytic subunit PRKACA at the cell membrane, preventing PRKACA-mediated phosphorylation of GLI transcription factors which releases the GLI proteins from PRKACA-mediated inhibition and allows for transcriptional activation of hedgehog pathway target genes (PubMed:33886552). Required for the accumulation of KIF7, GLI2 and GLI3 in the cilia. Interacts with DLG5 at the ciliary base to induce the accumulation of KIF7 and GLI2 at the ciliary tip for GLI2 activation (PubMed:25644602).
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Uniprot ID
P56726
Ensembl ID
ENSG00000128602
Subcellular Location
Cell membrane
Cell projection
Cilium
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: CL001023 , 3T3/HH FlashII-7
Compound ID Compound Name Compound Formula
CP0429582
LY-2940680
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C26H24F4N6O
 1
1
IC50 = 1.18 nM
   TI
   LI
   LO
   TS
CP0495141
1-[4-[5-chloro-2-(oxan-4-ylamino)pyrimidin-4-yl]sulfanylphenyl]-3-[1-[4,5-dimethyl-6-(2-methylpyrazol-3-yl)pyridazin-3-yl]piperidin-4-yl]urea
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C31H37ClN10O2S
 1
1
IC50 = 17.59 nM
   TI
   LI
   LO
   TS
CP0569869
1-[4-[5-chloro-2-[(1-methylpyrazol-4-yl)amino]pyrimidin-4-yl]oxyphenyl]-3-[1-[4,5-dimethyl-6-(2-methylpyrazol-3-yl)pyridazin-3-yl]piperidin-4-yl]urea
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C30H33ClN12O2
 1
1
IC50 = 17.79 nM
   TI
   LI
   LO
   TS
CP0570817
1-[4-[[5-chloro-2-(oxan-4-ylamino)pyrimidin-4-yl]amino]phenyl]-3-[1-[4,5-dimethyl-6-(2-methylpyrazol-3-yl)pyridazin-3-yl]piperidin-4-yl]urea
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C31H38ClN11O2
 1
1
IC50 = 63.92 nM
   TI
   LI
   LO
   TS
CP0571974
1-[1-[4,5-dimethyl-6-(2-methylpyrazol-3-yl)pyridazin-3-yl]piperidin-4-yl]-3-[4-[5-methyl-2-(oxan-4-ylamino)pyrimidin-4-yl]oxyphenyl]urea
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C32H40N10O3
 1
1
IC50 = 149.65 nM
   TI
   LI
   LO
   TS
CP0260228
1-[1-[4,5-dimethyl-6-(2-methylpyrazol-3-yl)pyridazin-3-yl]piperidin-4-yl]-3-[4-[2-(oxan-4-ylamino)-5-(trifluoromethyl)pyrimidin-4-yl]sulfanylphenyl]urea
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C32H37F3N10O2S
 1
1
IC50 = 154.9 nM
   TI
   LI
   LO
   TS
CP0575442
1-[1-[4,5-dimethyl-6-(2-methylpyrazol-3-yl)pyridazin-3-yl]piperidin-4-yl]-3-[4-[2-(oxan-4-ylamino)-5-(trifluoromethyl)pyrimidin-4-yl]oxyphenyl]urea
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C32H37F3N10O3
 1
1
IC50 = 190.3 nM
   TI
   LI
   LO
   TS
CP0488414
1-[4-[5-chloro-2-(oxan-4-ylamino)pyrimidin-4-yl]oxyphenyl]-3-[1-[4,5-dimethyl-6-(1-methylpyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]urea
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C31H37ClN10O3
 1
1
IC50 = 409.2 nM
   TI
   LI
   LO
   TS
CP0570816
1-[4-[5-chloro-2-(oxan-4-ylamino)pyrimidin-4-yl]oxyphenyl]-3-[1-[6-(1-methylpyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]urea
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C29H33ClN10O3
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0357751
N-[2,4-dimethyl-5-(1-methylimidazol-4-yl)phenyl]-4-(pyridin-2-ylmethoxy)benzamide
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C25H24N4O2
 1
1 EC50 = 3.1 nM
CP0134521
N-[5-(1H-imidazol-2-yl)-2,4-dimethylphenyl]-4-(pyridin-2-ylmethoxy)benzamide
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C24H22N4O2
 1
1 EC50 = 20 nM
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT04361 Protein smoothened Homo sapiens, Human