General Information of the Protein
Protein ID
PT00951
Protein Name
Proto-oncogene tyrosine-protein kinase receptor Ret
Secondarily
Protein Name
Cadherin family member 12
Proto-oncogene c-Ret
Gene Name
RET
Secondarily
Gene Name
CDHF12
CDHR16
PTC
RET51
Sequence
MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAPEEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLTVYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENRPPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELVAVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFDADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNRNLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFAQIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAELHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGRCEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPRGIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLKQVNHPHVIKLYGACSQDGPLLLIVEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVYEEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase Ret family
Function
Receptor tyrosine-protein kinase involved in numerous cellular mechanisms including cell proliferation, neuronal navigation, cell migration, and cell differentiation upon binding with glial cell derived neurotrophic factor family ligands. Phosphorylates PTK2/FAK1. Regulates both cell death/survival balance and positional information. Required for the molecular mechanisms orchestration during intestine organogenesis; involved in the development of enteric nervous system and renal organogenesis during embryonic life, and promotes the formation of Peyer's patch-like structures, a major component of the gut-associated lymphoid tissue. Modulates cell adhesion via its cleavage by caspase in sympathetic neurons and mediates cell migration in an integrin (e.g. ITGB1 and ITGB3)-dependent manner. Involved in the development of the neural crest. Active in the absence of ligand, triggering apoptosis through a mechanism that requires receptor intracellular caspase cleavage. Acts as a dependence receptor; in the presence of the ligand GDNF in somatotrophs (within pituitary), promotes survival and down regulates growth hormone (GH) production, but triggers apoptosis in absence of GDNF. Regulates nociceptor survival and size. Triggers the differentiation of rapidly adapting (RA) mechanoreceptors. Mediator of several diseases such as neuroendocrine cancers; these diseases are characterized by aberrant integrins-regulated cell migration. Mediates, through interaction with GDF15-receptor GFRAL, GDF15-induced cell-signaling in the brainstem which induces inhibition of food-intake. Activates MAPK- and AKT-signaling pathways (PubMed:28846097, PubMed:28953886, PubMed:28846099). Isoform 1 in complex with GFRAL induces higher activation of MAPK-signaling pathway than isoform 2 in complex with GFRAL (PubMed:28846099).
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Uniprot ID
Primary ID:
P07949

Secondarily ID:
A8K6Z2
Q15250
Q9BTB0
Q9H4A2
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Ensembl ID
ENSG00000165731
HGNC ID
HGNC:9967
Subcellular Location
Cell membrane
Endosome 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: CL000077 , Ba/F3
Compound ID Compound Name Compound Formula
CP0046394
BMS-907351
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C28H24FN3O5
 5
1
GI50 = 10 nM
   TI
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2
GI50 = 50 nM
   TI
   LI
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3
GI50 = 890 nM
   TI
   LI
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4
GI50 = 910 nM
   TI
   LI
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   TS
5
IC50 = 180 nM
   TI
   LI
   LO
   TS
CP0065824
3-(5-cyclopropyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C14H16N6O
 4
1
GI50 = 80 nM
   TI
   LI
   LO
   TS
2
GI50 = 90 nM
   TI
   LI
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3
GI50 = 320 nM
   TI
   LI
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4
GI50 = 500 nM
   TI
   LI
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   TS
CP0421231
N-[[1-[4-[[3-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]carbamoylamino]-2-(trifluoromethyl)phenyl]piperidin-4-yl]methyl]propanamide
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C34H36F3N5O5
 1
1
GI50 = 120 nM
   TI
   LI
   LO
   TS
CP0441015
N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]propanamide
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C30H31F3N6OS
 1
1
GI50 = 200 nM
   TI
   LI
   LO
   TS
CP0062729
3-(2-phenylethynyl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C16H15N5
 4
1
GI50 = 350 nM
   TI
   LI
   LO
   TS
2
GI50 = 610 nM
   TI
   LI
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3
GI50 = 2600 nM
   TI
   LI
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4
GI50 = 5430 nM
   TI
   LI
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CP0230028
3-(5-cyclopropyl-1,2-oxazol-3-yl)-1-(oxan-4-yl)pyrazolo[3,4-d]pyrimidin-4-amine
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C16H18N6O2
 2
1
GI50 = 440 nM
   TI
   LI
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   TS
2
GI50 = 1930 nM
   TI
   LI
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CP0156701
1-cyclohexyl-3-(5-cyclopropyl-1,2-oxazol-3-yl)pyrazolo[3,4-d]pyrimidin-4-amine
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C17H20N6O
 2
1
GI50 = 520 nM
   TI
   LI
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2
GI50 = 2000 nM
   TI
   LI
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CP0065873
1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]-2-(dimethylamino)ethanone
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C26H29N7O2
 1
1
GI50 = 650 nM
   TI
   LI
   LO
   TS
CP0140879
1-propan-2-yl-3-(5-pyridin-2-yl-1,2-oxazol-3-yl)pyrazolo[3,4-d]pyrimidin-4-amine
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C16H15N7O
 2
1
GI50 = 700 nM
   TI
   LI
   LO
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2
GI50 = 1110 nM
   TI
   LI
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CP0156708
3-(5-ethyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C13H16N6O
 2
1
GI50 = 1560 nM
   TI
   LI
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2
GI50 = 5770 nM
   TI
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CP0364644
1-[4-amino-3-(5-cyclopropyl-1,2-oxazol-3-yl)pyrazolo[3,4-d]pyrimidin-1-yl]-2-methylpropan-2-ol
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C15H18N6O2
 2
1
GI50 = 1770 nM
   TI
   LI
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2
GI50 = 6750 nM
   TI
   LI
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   TS
CP0083897
1-propan-2-yl-3-(5-propan-2-yl-1,2-oxazol-3-yl)pyrazolo[3,4-d]pyrimidin-4-amine
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C14H18N6O
 2
1
GI50 = 2400 nM
   TI
   LI
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2
GI50 = 5900 nM
   TI
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CP0095871
3-(5-cyclopropyl-1,2-oxazol-3-yl)-1-methylpyrazolo[3,4-d]pyrimidin-4-amine
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C12H12N6O
 2
1
GI50 = 2670 nM
   TI
   LI
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2
GI50 = 5560 nM
   TI
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CP0106777
3-(1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C11H12N6O
 2
1
GI50 = 3210 nM
   TI
   LI
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2
GI50 = 8940 nM
   TI
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CP0304455
3-(5-phenyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C17H16N6O
 2
1
GI50 = 3460 nM
   TI
   LI
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   TS
2
GI50 = 4970 nM
   TI
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   TS
CP0071780
3-(5-cyclohexyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C17H22N6O
 2
1
GI50 = 4730 nM
   TI
   LI
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2
GI50 = 9500 nM
   TI
   LI
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CP0089052
3-(5-cyclopropyl-1,2-oxazol-3-yl)-2H-pyrazolo[3,4-d]pyrimidin-4-amine
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C11H10N6O
 2
1
GI50 = 5340 nM
   TI
   LI
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   TS
2
GI50 > 10000 nM
   TI
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CP0174992
3-(5-tert-butyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C15H20N6O
 2
1
GI50 = 6120 nM
   TI
   LI
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2
GI50 = 7310 nM
   TI
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CP0309740
3-(5-phenyl-4,5-dihydro-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C17H18N6O
 2
1
GI50 = 6240 nM
   TI
   LI
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2
GI50 > 10000 nM
   TI
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CP0198875
3-(5-cyclopentyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C16H20N6O
 2
1
GI50 = 7120 nM
   TI
   LI
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2
GI50 > 10000 nM
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CP0198308
3-[(E)-phenylmethoxyiminomethyl]-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C16H18N6O
 2
1
GI50 = 7410 nM
   TI
   LI
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2
GI50 > 10000 nM
   TI
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CP0095875
1-benzyl-3-(5-cyclopropyl-1,2-oxazol-3-yl)pyrazolo[3,4-d]pyrimidin-4-amine
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C18H16N6O
 1
1
GI50 > 10000 nM
   TI
   LI
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CP0174991
3-(5-benzyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C18H18N6O
 1
1
GI50 > 10000 nM
   TI
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CP0174993
3-(5-cyclopropyl-1,2-oxazol-3-yl)-1-heptylpyrazolo[3,4-d]pyrimidin-4-amine
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C18H24N6O
 1
1
GI50 > 10000 nM
   TI
   LI
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CP0181070
3-[5-(4-fluorophenyl)-1,2-oxazol-3-yl]-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C17H15FN6O
 1
1
GI50 > 10000 nM
   TI
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CP0401663
(NE)-N-[(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)methylidene]hydroxylamine
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C9H12N6O
 1
1
GI50 > 10000 nM
   TI
   LI
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CP0061016
3-(4-Amino-7-cyclopentyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-phenol
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C17H18N4O
 1
1
IC50 = 4 nM
   TI
   LI
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CP0388620
methyl N-[4-[7-amino-3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxypyrazolo[1,5-a]pyrimidin-6-yl]phenyl]carbamate
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C28H32N6O5
 1
1
IC50 = 6 nM
   TI
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CP0418567
3-[4-amino-7-[3-(hydroxymethyl)cyclobutyl]pyrrolo[2,3-d]pyrimidin-5-yl]phenol
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C17H18N4O2
 1
1
IC50 = 51 nM
   TI
   LI
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CP0165616
N-[3-(1,3-benzodioxol-5-yl)pyrazolo[1,5-a]pyrimidin-5-yl]-N',N'-dimethylpropane-1,3-diamine
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C18H21N5O2
 2
1
IC50 = 110 nM
   TI
   LI
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2
IC50 = 4000 nM
   TI
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CP0388616
3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxy-6-phenylpyrazolo[1,5-a]pyrimidin-7-amine
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C26H29N5O3
 1
1
IC50 = 170 nM
   TI
   LI
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CP0388615
3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxy-6-(1,3-thiazol-2-yl)pyrazolo[1,5-a]pyrimidin-7-amine
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C23H26N6O3S
 1
1
IC50 = 210 nM
   TI
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CP0081362
4-fluoro-2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-(3-methyl-2H-indazol-5-yl)pyridin-2-yl]phenol
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C27H23FN4O2
 1
1
IC50 = 315.7 nM
   TI
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CP0356495
N-[3-(1,3-benzodioxol-5-yl)pyrazolo[1,5-a]pyrimidin-5-yl]-N',N'-dimethylethane-1,2-diamine
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C17H19N5O2
 1
1
IC50 = 740 nM
   TI
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CP0138866
1-[4-[3-[4-amino-5-(2-fluoro-5-hydroxyphenyl)pyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl]piperazin-1-yl]ethanone
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C22H25FN6O2
 1
1
IC50 = 920 nM
   TI
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CP0476295
3-(1,3-benzodioxol-5-yl)-N-(pyridin-2-ylmethyl)pyrazolo[1,5-a]pyrimidin-5-amine
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C19H15N5O2
 1
1
IC50 = 1100 nM
   TI
   LI
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CP0225753
3-(1,3-benzodioxol-5-yl)-N-(piperidin-4-ylmethyl)pyrazolo[1,5-a]pyrimidin-5-amine
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C19H21N5O2
 1
1
IC50 = 1300 nM
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CP0019908
BDBM50242742
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C30H40ClN7O3S
 1
1
IC50 = 1385 nM
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CP0037988
N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-amine
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C22H24BrFN4O2
 1
1
IC50 = 1500 nM
   TI
   LI
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CP0356492
3-(1,3-benzodioxol-5-yl)-N-(pyridin-4-ylmethyl)pyrazolo[1,5-a]pyrimidin-5-amine
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C19H15N5O2
 1
1
IC50 = 1500 nM
   TI
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CP0225749
3-(1H-indazol-6-yl)-N-(pyridin-4-ylmethyl)pyrazolo[1,5-a]pyrimidin-5-amine
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C19H15N7
 1
1
IC50 = 2800 nM
   TI
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CP0661487
3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea monophosphate
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C26H34Cl2N7O7P
 1
1
IC50 = 3352 nM
   TI
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CP0385508
2-[4-[4-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperazin-1-yl]acetic acid
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C27H28FN7O2
 1
1
IC50 = 3700 nM
   TI
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CP0462095
4-[5-(pyridin-2-ylmethylamino)pyrazolo[1,5-a]pyrimidin-3-yl]benzamide
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C19H16N6O
 1
1
IC50 = 3700 nM
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CP0237973
4-[5-(pyridin-3-ylmethylamino)pyrazolo[1,5-a]pyrimidin-3-yl]benzamide
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C19H16N6O
 1
1
IC50 = 3900 nM
   TI
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CP0551221
4-[5-(pyridin-4-ylmethylamino)pyrazolo[1,5-a]pyrimidin-3-yl]benzamide
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C19H16N6O
 1
1
IC50 = 4400 nM
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CP0388864
4-[6-(benzylamino)imidazo[1,2-b]pyridazin-3-yl]benzonitrile
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C20H15N5
 1
1
IC50 = 4900 nM
   TI
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CP0385511
1-[4-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperidin-4-ol
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C26H27FN6O
 1
1
IC50 = 6000 nM
   TI
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CP0088325
2-[[3-(1,3-benzodioxol-5-yl)pyrazolo[1,5-a]pyrimidin-5-yl]amino]ethanol
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C15H14N4O3
 1
1
IC50 = 6800 nM
   TI
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CP0395047
6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]-3-pyridin-2-ylimidazo[1,2-b]pyridazine
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C21H18FN5
 1
1
IC50 = 8000 nM
   TI
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CP0160448
4-[5-(pyridin-4-ylmethylamino)pyrazolo[1,5-a]pyrimidin-3-yl]benzenesulfonamide
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C18H16N6O2S
 1
1
IC50 > 10000 nM
   TI
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CP0575427
4-[5-[2-(dimethylamino)ethylamino]pyrazolo[1,5-a]pyrimidin-3-yl]benzamide
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C17H20N6O
 1
1
IC50 > 10000 nM
   TI
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0019908
BDBM50242742
   Show/Hide
C30H40ClN7O3S
 4
1 EC50 > 1000 nM
2 Kd = 120 nM
3 Kd = 140 nM
4 Kd = 150 nM
CP0037988
N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-amine
   Show/Hide
C22H24BrFN4O2
 14
1 IC50 = 0.13 nM
2 IC50 = 7 nM
3 IC50 = 9 nM
4 IC50 = 100 nM
5 IC50 = 102 nM
6 IC50 = 130 nM
7 IC50 = 950 nM
8 IC50 = 2049 nM
9 IC50 = 2597 nM
10 IC50 = 3597 nM
11 IC50 > 5000 nM
12 Kd = 14 nM
13 Kd = 34 nM
14 Kd > 10000 nM
CP0081362
4-fluoro-2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-(3-methyl-2H-indazol-5-yl)pyridin-2-yl]phenol
   Show/Hide
C27H23FN4O2
 1
1 IC50 = 0.2 nM
CP0244732
N-[4-(2-amino-2-methylpropyl)-3-(trifluoromethyl)phenyl]-2-[4-(4-ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]acetamide
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C26H27F4N3O3
 1
1 IC50 = 0.2 nM
CP0035428
3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide
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C29H27F3N6O
 5
1 IC50 = 0.3 nM
2 IC50 = 0.9 nM
3 IC50 = 7 nM
4 IC50 = 25.8 nM
5 IC50 = 33.9 nM
CP0097084
2-[4-(4-ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]-N-[4-(2-hydroxy-2-methylpropyl)-3-(trifluoromethyl)phenyl]acetamide
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C26H26F4N2O4
 1
1 IC50 = 0.4 nM
CP0189108
2-(4-(4-Ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl)-N-(4-(3-hydroxy-2,2-dimethylpropyl)-3-(trifluoromethyl)phenyl)acetamide
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C27H28F4N2O4
 1
1 IC50 = 0.4 nM
CP0213933
2-(4-(4-Ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl)-N-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)acetamide
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C22H21F4N3O4
 2
1 IC50 = 0.4 nM
2 IC50 <= 100 nM
CP0242634
2-[4-(4-ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]-N-[3-(5-methyl-1,3,4-oxadiazol-2-yl)-5-(trifluoromethyl)phenyl]acetamide
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C25H20F4N4O4
 1
1 IC50 = 0.4 nM
CP0268012
2-(4-(4-Ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl)-N-(3-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-5-yl)acetamide
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C22H21F4N3O4
 2
1 IC50 = 0.4 nM
2 IC50 <= 100 nM
CP0535057
US10112942, Example 163
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C29H31N7O3
 3
1 IC50 = 0.4 nM
2 IC50 = 0.42 nM
3 IC50 = 0.7 nM
CP0004106
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one
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C28H26N4O3
 9
1 IC50 = 0.46 nM
2 IC50 = 1.69 nM
3 IC50 = 2.03 nM
4 IC50 = 3.43 nM
5 IC50 = 4.6 nM
6 IC50 = 4.7 nM
7 Kd = 12 nM
8 Kd = 15 nM
9 Kd = 28 nM
CP0138866
CHEMBL4854822
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C22H25FN6O2
 1
1 IC50 = 0.54 nM
CP0242633
N-[4-(2,2-dimethyl-3-methylsulfonylpropyl)-3-(trifluoromethyl)phenyl]-2-[4-(4-ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]acetamide
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C28H30F4N2O5S
 1
1 IC50 = 0.6 nM
CP0189107
N-[4-(1-cyanoethyl)-3-(trifluoromethyl)phenyl]-2-[4-(4-ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]acetamide
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C25H21F4N3O3
 1
1 IC50 = 0.7 nM
CP0242632
N-[4-[(dimethylamino)methyl]-3-(trifluoromethyl)phenyl]-2-[4-(4-ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]acetamide
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C25H25F4N3O3
 1
1 IC50 = 0.8 nM
CP0002211
N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
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C22H27FN4O2
 9
1 IC50 < 1 nM
2 IC50 = 5 nM
3 IC50 = 220 nM
4 IC50 = 224 nM
5 Kd = 5.8 nM
6 Kd = 8.7 nM
7 Kd = 12 nM
8 Kd = 13 nM
9 Kd = 19 nM
CP0065824
3-(5-cyclopropyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C14H16N6O
 7
1 IC50 = 1.4 nM
2 IC50 = 2 nM
3 IC50 = 3 nM
4 IC50 = 4 nM
5 IC50 = 6 nM
6 IC50 = 10 nM
7 IC50 = 21 nM
CP0124203
2-(4-(4-Ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl)-N-(3-(trifluoromethyl)phenyl)acetamide
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C22H18F4N2O3
 1
1 IC50 = 1.7 nM
CP0156701
1-cyclohexyl-3-(5-cyclopropyl-1,2-oxazol-3-yl)pyrazolo[3,4-d]pyrimidin-4-amine
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C17H20N6O
 2
1 IC50 = 2 nM
2 IC50 = 14 nM
CP0113988
CEP-32496
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C24H22F3N5O5
 8
1 IC50 = 2 nM
2 IC50 = 4 nM
3 IC50 = 4.34 nM
4 IC50 = 7 nM
5 IC50 = 31 nM
6 IC50 = 168 nM
7 IC50 = 319 nM
8 Kd = 1.5 nM
CP0046394
BMS-907351
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C28H24FN3O5
 18
1 IC50 = 2.4 nM
2 IC50 = 4 nM
3 IC50 = 5 nM
4 IC50 = 5.2 nM
5 IC50 = 7 nM
6 IC50 = 8 nM
7 IC50 = 10.1 nM
8 IC50 = 13 nM
9 IC50 = 14 nM
10 IC50 = 16 nM
11 IC50 = 18 nM
12 IC50 = 37 nM
13 IC50 = 45 nM
14 IC50 = 76 nM
15 IC50 = 132 nM
16 IC50 = 230 nM
17 IC50 = 358 nM
18 IC50 = 1500 nM
CP0329627
N-[3-[(dimethylamino)methyl]-2-fluoro-5-(trifluoromethyl)phenyl]-2-[4-(4-ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]acetamide
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C25H24F5N3O3
 1
1 IC50 = 2.8 nM
CP0041572
BDBM50249542
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C22H23FN6O5
 4
1 IC50 = 5 nM
2 Kd = 2.2 nM
3 Kd = 3.1 nM
4 Kd = 4.1 nM
CP0230028
3-(5-cyclopropyl-1,2-oxazol-3-yl)-1-(oxan-4-yl)pyrazolo[3,4-d]pyrimidin-4-amine
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C16H18N6O2
 2
1 IC50 = 5 nM
2 IC50 = 41 nM
CP0018477
4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)phenoxy]-N-methylpyridine-2-carboxamide
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C21H16ClF3N4O3
 9
1 IC50 = 5.9 nM
2 IC50 = 6 nM
3 IC50 = 9 nM
4 IC50 = 11 nM
5 Kd = 7.4 nM
6 Kd = 13 nM
7 Kd = 22 nM
8 Kd = 39 nM
9 Kd = 62 nM
CP0062729
3-(2-phenylethynyl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C16H15N5
 8
1 IC50 = 8 nM
2 IC50 = 14 nM
3 IC50 = 54 nM
4 IC50 = 56.5 nM
5 IC50 = 57 nM
6 IC50 = 75 nM
7 IC50 = 2650 nM
8 IC50 = 3130 nM
CP0488635
N-cyclopropyl-2-[4-[[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]amino]phenyl]acetamide
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C24H31N9O
 1
1 IC50 = 12.32 nM
CP0547123
N-(4-fluorophenyl)-2-[4-[[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]amino]phenyl]acetamide
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C27H30FN9O
 1
1 IC50 = 13.14 nM
CP0260646
N-(3-fluorophenyl)-2-[4-[[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]amino]phenyl]acetamide
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C27H30FN9O
 1
1 IC50 = 18.68 nM
CP0165616
N-[3-(1,3-benzodioxol-5-yl)pyrazolo[1,5-a]pyrimidin-5-yl]-N',N'-dimethylpropane-1,3-diamine
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C18H21N5O2
 1
1 IC50 = 19 nM
CP0551221
4-[5-(pyridin-4-ylmethylamino)pyrazolo[1,5-a]pyrimidin-3-yl]benzamide
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C19H16N6O
 1
1 IC50 = 20 nM
CP0578756
3-[(4-methoxyquinolin-3-yl)diazenyl]-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide
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C30H29F3N6O2
 1
1 IC50 = 24 nM
CP0095871
3-(5-cyclopropyl-1,2-oxazol-3-yl)-1-methylpyrazolo[3,4-d]pyrimidin-4-amine
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C12H12N6O
 2
1 IC50 = 27 nM
2 IC50 = 182 nM
CP0476295
3-(1,3-benzodioxol-5-yl)-N-(pyridin-2-ylmethyl)pyrazolo[1,5-a]pyrimidin-5-amine
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C19H15N5O2
 1
1 IC50 = 39 nM
CP0083897
1-propan-2-yl-3-(5-propan-2-yl-1,2-oxazol-3-yl)pyrazolo[3,4-d]pyrimidin-4-amine
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C14H18N6O
 2
1 IC50 = 41 nM
2 IC50 = 355 nM
CP0156708
3-(5-ethyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C13H16N6O
 2
1 IC50 = 41 nM
2 IC50 = 531 nM
CP0181446
5-amino-3-(5-cyclopropyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazole-4-carboxamide
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C13H17N5O2
 1
1 IC50 = 44 nM
CP0462095
4-[5-(pyridin-2-ylmethylamino)pyrazolo[1,5-a]pyrimidin-3-yl]benzamide
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C19H16N6O
 1
1 IC50 = 44 nM
CP0237973
4-[5-(pyridin-3-ylmethylamino)pyrazolo[1,5-a]pyrimidin-3-yl]benzamide
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C19H16N6O
 1
1 IC50 = 51 nM
CP0089052
3-(5-cyclopropyl-1,2-oxazol-3-yl)-2H-pyrazolo[3,4-d]pyrimidin-4-amine
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C11H10N6O
 2
1 IC50 = 52 nM
2 IC50 = 354 nM
CP0364644
1-[4-amino-3-(5-cyclopropyl-1,2-oxazol-3-yl)pyrazolo[3,4-d]pyrimidin-1-yl]-2-methylpropan-2-ol
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C15H18N6O2
 2
1 IC50 = 68 nM
2 IC50 = 217 nM
CP0095875
1-benzyl-3-(5-cyclopropyl-1,2-oxazol-3-yl)pyrazolo[3,4-d]pyrimidin-4-amine
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C18H16N6O
 2
1 IC50 = 74 nM
2 IC50 = 557 nM
CP0160838
5-amino-1-propan-2-yl-3-(5-thiophen-2-yl-1,2-oxazol-3-yl)pyrazole-4-carboxamide
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C14H15N5O2S
 1
1 IC50 = 78 nM
CP0356495
N-[3-(1,3-benzodioxol-5-yl)pyrazolo[1,5-a]pyrimidin-5-yl]-N',N'-dimethylethane-1,2-diamine
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C17H19N5O2
 1
1 IC50 = 91 nM
CP0174993
3-(5-cyclopropyl-1,2-oxazol-3-yl)-1-heptylpyrazolo[3,4-d]pyrimidin-4-amine
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C18H24N6O
 2
1 IC50 = 96 nM
2 IC50 = 927 nM
CP0483382
2-(4-(5-Ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2,3-difluorophenyl)-N-(4-(2-hydroxyethoxy)-3-(trifluoromethyl)phenyl)acetamide
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C24H21F5N2O5
 1
1 IC50 <= 100 nM
CP0088325
2-[[3-(1,3-benzodioxol-5-yl)pyrazolo[1,5-a]pyrimidin-5-yl]amino]ethanol
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C15H14N4O3
 1
1 IC50 = 130 nM
CP0181070
3-[5-(4-fluorophenyl)-1,2-oxazol-3-yl]-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C17H15FN6O
 1
1 IC50 = 150 nM
CP0181447
5-amino-1-propan-2-yl-3-(5-thiophen-3-yl-1,2-oxazol-3-yl)pyrazole-4-carboxamide
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C14H15N5O2S
 1
1 IC50 = 162 nM
CP0304455
3-(5-phenyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C17H16N6O
 1
1 IC50 = 190 nM
CP0225753
3-(1,3-benzodioxol-5-yl)-N-(piperidin-4-ylmethyl)pyrazolo[1,5-a]pyrimidin-5-amine
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C19H21N5O2
 1
1 IC50 = 200 nM
CP0213044
N-(5-tert-butyl-1,2-oxazol-3-yl)-2-(4-imidazo[1,2-a]pyridin-6-ylphenyl)acetamide
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C22H22N4O2
 4
1 IC50 = 210 nM
2 IC50 = 380 nM
3 IC50 = 420 nM
4 IC50 = 440 nM
CP0174992
3-(5-tert-butyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C15H20N6O
 2
1 IC50 = 210 nM
2 IC50 = 2100 nM
CP0106777
3-(1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C11H12N6O
 2
1 IC50 = 213 nM
2 IC50 = 903 nM
CP0174991
3-(5-benzyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C18H18N6O
 2
1 IC50 = 241 nM
2 IC50 = 1990 nM
CP0198875
3-(5-cyclopentyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C16H20N6O
 2
1 IC50 = 241 nM
2 IC50 = 1570 nM
CP0356492
3-(1,3-benzodioxol-5-yl)-N-(pyridin-4-ylmethyl)pyrazolo[1,5-a]pyrimidin-5-amine
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C19H15N5O2
 1
1 IC50 = 290 nM
CP0225749
3-(1H-indazol-6-yl)-N-(pyridin-4-ylmethyl)pyrazolo[1,5-a]pyrimidin-5-amine
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C19H15N7
 1
1 IC50 = 300 nM
CP0575427
4-[5-[2-(dimethylamino)ethylamino]pyrazolo[1,5-a]pyrimidin-3-yl]benzamide
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C17H20N6O
 1
1 IC50 = 350 nM
CP0160448
4-[5-(pyridin-4-ylmethylamino)pyrazolo[1,5-a]pyrimidin-3-yl]benzenesulfonamide
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C18H16N6O2S
 1
1 IC50 = 360 nM
CP0569365
3-[(4-methoxyquinolin-3-yl)diazenyl]-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide
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C30H29F3N6O2
 1
1 IC50 = 363 nM
CP0309740
3-(5-phenyl-4,5-dihydro-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C17H18N6O
 2
1 IC50 = 583 nM
2 IC50 = 5680 nM
CP0121027
N-(5-tert-butyl-1,2-oxazol-3-yl)-2-(3-imidazo[1,2-b]pyridazin-6-yloxyphenyl)acetamide
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C21H21N5O3
 1
1 IC50 = 750 nM
CP0071780
3-(5-cyclohexyl-1,2-oxazol-3-yl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C17H22N6O
 1
1 IC50 = 910 nM
CP0140879
1-propan-2-yl-3-(5-pyridin-2-yl-1,2-oxazol-3-yl)pyrazolo[3,4-d]pyrimidin-4-amine
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C16H15N7O
 2
1 IC50 = 910 nM
2 IC50 = 5880 nM
CP0401663
(NE)-N-[(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)methylidene]hydroxylamine
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C9H12N6O
 2
1 IC50 = 3680 nM
2 IC50 = 4900 nM
CP0198308
3-[(E)-phenylmethoxyiminomethyl]-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine
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C16H18N6O
 1
1 IC50 = 8330 nM
CP0483381
N-(3,4-dichlorophenyl)-2-[4-(5-ethoxy-6-oxo-1H-pyridin-3-yl)-2-fluorophenyl]acetamide
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C21H17Cl2FN2O3
 1
1 IC50 >= 100 nM
CP0661487
3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea monophosphate
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C26H34Cl2N7O7P
 1
1 IC50 > 10000 nM
Clinical Information about the Protein
Target 1 ( Proto-oncogene c-Ret (RET) )
Target Type Successful Target
Disease 6 Target-related Diseases  6
1 Acute lymphoblastic leukaemia [ICD-11: 2A85]
2 Metastatic colorectal cancer [ICD-11: 2B91]
3 Thrombocytopenia [ICD-11: 3B64]
4 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
5 Inflammatory bowel disease [ICD-11: DD72]
6 Non-small-cell lung cancer [ICD-11: 2C25.Y]
Approved Drug(s) 5 Approved Drugs  5
1 Ponatinib Approved
Acute lymphoblastic leukaemia
2 Regorafenib Approved
Metastatic colorectal cancer
3 Romiplostim Approved
Thrombocytopenia
4 Vandetanib Approved
Solid tumour/cancer
5 Pralsetinib Approved
Non-small-cell lung cancer
Clinical Trial Drug(s) 4 Clinical Trial Drugs  4
1 CEP-32496 Phase 1/2
Solid tumour/cancer
2 MGCD516 Phase 2/3
Solid tumour/cancer
3 GSK3179106 Phase 1
Inflammatory bowel disease
4 tamatinib Clinical trial
Solid tumour/cancer
Target 2 ( RET G691S mutant (RET G691S) )
Target Type Patented-recorded Target
Target 3 ( RET M918T mutant (RET M918T) )
Target Type Patented-recorded Target
Target 4 ( RET S891A mutant (RET S891A) )
Target Type Patented-recorded Target
Target 5 ( RET V804L mutant (RET V804L) )
Target Type Patented-recorded Target
Target 6 ( RET V804M mutant (RET V804M) )
Target Type Patented-recorded Target
Target 7 ( RET Y791F mutant (RET Y791F) )
Target Type Patented-recorded Target
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT06733 Proto-oncogene tyrosine-protein kinase receptor Ret Mus musculus, Mouse