Reaction Details
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GTPase KRas [G12D]
Ligand
BDBM573644
Substrate
n/a
Meas. Tech.
Inhibition of KRas G12D-mediated Phosphorylation of ERK
IC50
0.400±n/a nM
Citation
Wang, X; Burns, AC; Christensen, JG; Ketcham, JM; Lawson, JD; Marx, MA; Smith, CR; Allen, S; Blake, JF; Chicarelli, MJ; Dahlke, JR; Dai, D; Fell, JB; Fischer, JP; Mejia, MJ; Newhouse, B; Nguyen, P; O''Leary, JM; Pajk, S; Rodriguez, ME; Savechenkov, P; Tang, TP; Vigers, GP; Zhao, Q; Kahn, DR; Gaudino, J; Hilton, MC KRAS G12D INHIBITORS US Patent US20230279025 Publication Date 9/7/2023 More Info.:
Target
Name:
GTPase KRas [G12D]
Synonyms:
GTPase KRas (G12D) | KRAS | KRAS2 | RASK2 | RASK_HUMAN
Type:
Enzyme Catalytic Domain
Mol. Mass.:
21713.12
Organism:
Homo sapiens (Human)
Description:
P01116[G12D]
Residue:
189
Sequence:
MTEYKLVVVGADGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
Inhibitor
Name:
BDBM573644
Synonyms:
US11453683, Example 439 | US20230279025, Example 439
Type:
Small organic molecule
Emp. Form.:
C37H39F2N7O3
Mol. Mass.:
667.7475
SMILES:
CN(C)C(=O)OC[C@H]1CC[C@@]2(COc3nc(N4CC5CCC(C4)N5)c4cnc(c(F)c4n3)-c3cccc4ccc(F)c(C#C)c34)CCCN12 |r|
Structure:
