Ki Summary

Reaction Details

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Target

Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]

Ligand

BDBM296824

Substrate/Competitor

n/a

Meas. Tech.

RET G810R Mutant Assay

IC50

302±n/a nM

Citation

Andrews, SW; Aronow, S; Blake, JF; Brandhuber, BJ; Cook, A; Haas, J; Jiang, Y; Kolakowski, GR; McFaddin, EA; McKenney, ML; McNulty, OT; Metcalf, AT; Moreno, DA; Tang, TP; Ren, L Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors US Patent US10555944 Publication Date 2/11/2020

More Info.:

Get all data from this article, Assay Method

Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]

Name:

Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]

Synonyms:

CDHF12 | CDHR16 | PTC | Proto-oncogene tyrosine-protein kinase receptor Ret (G810R) | RET | RET51 | RET_HUMAN

Type:

Enzyme Catalytic Domain

Mol. Mass.:

51635.31

Organism:

Homo sapiens (Human)

Description:

P07949[658-1114,G810R]

Residue:

457

Sequence:

HCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKW
EFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFN
VLKQVNHPHVIKLYGACSQDGPLLLIVEYAKYRSLRGFLRESRKVGPGYLGSGGSRNSSS
LDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSR
DVYEEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPP
ERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLD
LAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPL
TRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS

BDBM296824

n/a

Name

BDBM296824

Synonyms:

6-ethoxy-4-(5-(6-((6- methoxy-5- methylpyridin-3- yl)methyl)-3,6- diazabicyclo[3.1.1] heptan-3-yl)pyrazin-2- yl)pyrazolo[1,5- a]pyridine-3- carbonitrile | US10112942, Example 559 | US10137124, Example 559 | US10172851, Example 559 | US10555944, Example 559 | US10953005, Example 559

Type

Small organic molecule

Emp. Form.

C27H28N8O2

Mol. Mass.

496.5636

SMILES

CCOc1cc(-c2cnc(cn2)N2CC3CC(C2)N3Cc2cnc(OC)c(C)c2)c2c(cnn2c1)C#N

Structure