Reaction Details
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GTPase KRas [1-169,G12C,C118A]/Son of sevenless homolog 1 [564-1049]
Ligand
BDBM653488
Substrate
n/a
Meas. Tech.
Coupled Nucleotide Exchange Assay
IC50
87.0±n/a nM
Citation
LANMAN, BA; BANERJEE, A; CHU-MOYER, M; DAI, D; ESHON, J; HUANG, D; KALLER, MR; LEE, H; LOPEZ, P; MA, VV; MANONI, F; MEDINA, JM; PICKRELL, AJ; STELLWAGEN, JC; SUN, Z; TAMAYO, NA; ZHANG, W; ZHU, K HETEROCYCLIC SPIRO COMPOUNDS AND METHODS OF USE US Patent US20240059703 Publication Date 2/22/2024 More Info.:
Target
Name:
GTPase KRas [1-169,G12C,C118A]/Son of sevenless homolog 1 [564-1049]
Synonyms:
KRAS/SOS1
Type:
Protein
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
GTPase KRas
Synonyms:
GTPase KRas, N-terminally processed | K-Ras 2 | Ki-Ras | c-K-ras | c-Ki-ras | RASK_HUMAN | KRAS | KRAS2 | RASK2
Type:
PROTEIN
Mol. Mass.:
21656.10
Organism:
Human
Description:
ChEMBL_1476955
Residue:
189
Sequence:
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
Component 2
Name:
Son of sevenless homolog 1 [564-1049]
Synonyms:
Son of sevenless homolog 1 (SOS1)(564-1049) | SOS1_HUMAN | SOS1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
56970.22
Organism:
Human
Description:
aa 564-1049
Residue:
486
Sequence:
EEQMRLPSADVYRFAEPDSEENIIFEENMQPKAGIPIIKAGTVIKLIERLTYHMYADPNFVRTFLTTYRSFCKPQELLSLIIERFEIPEPEPTEADRIAIENGDQPLSAELKRFRKEYIQPVQLRVLNVCRHWVEHHFYDFERDAYLLQRMEEFIGTVRGKAMKKWVESITKIIQRKKIARDNGPGHNITFQSSPPTVEWHISRPGHIETFDLLTLHPIEIARQLTLLESDLYRAVQPSELVGSVWTKEDKEINSPNLLKMIRHTTNLTLWFEKCIVETENLEERVAVVSRIIEILQVFQELNNFNGVLEVVSAMNSSPVYRLDHTFEQIPSRQKKILEEAHELSEDHYKKYLAKLRSINPPCVPFFGIYLTNILKTEEGNPEVLKRHGKELINFSKRRKVAEITGEIQQYQNQPYCLRVESDIKRFFENLNPMGNSMEKEFTDYLFNKSLEIEPRNPKPLPRFPKKYSYPLKSPGVRPSNPRPGT
Inhibitor
Name:
BDBM653488
Synonyms:
US20240059703, Example 23-19 | 4-(2-chlorophenyl)-7-(4-methyl-1,3- thiazol-5-yl)-2-(2-(2-propenoyl)-2,6- diazaspiro[3.4]octan-6-yl)-5,6-dihydro-3- quinolinecarbonitrile | US20240059703, Example 23-42 | US20240059703, Example 23-41
Type:
Small organic molecule
Emp. Form.:
TBD
Mol. Mass.:
TBD
SMILES:
TBD
