Approval Year
| Substance Class |
Protein
Created
by
admin
on
Edited
Sat Dec 16 15:06:02 UTC 2023
by
admin
on
Sat Dec 16 15:06:02 UTC 2023
|
| Protein Type | SIGNAL TRANSDUCER (GTPASE) |
| Protein Sub Type | RAS |
| Sequence Origin | HUMAN |
| Sequence Type | COMPLETE |
| Record UNII |
ES4I8456YD
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
P01116
Created by
admin on Sat Dec 16 15:06:02 UTC 2023 , Edited by admin on Sat Dec 16 15:06:02 UTC 2023
|
PRIMARY | |||
|
ES4I8456YD
Created by
admin on Sat Dec 16 15:06:02 UTC 2023 , Edited by admin on Sat Dec 16 15:06:02 UTC 2023
|
PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
INHIBITOR -> TARGET |
Pre-clinical
|
||
|
|
INHIBITOR -> TARGET |
Binds to the switch II pocket of the KRAS G12C covalently reactive with cysteine 12 and locks KRAS G12C protein in its GDP-bound inactive form. LY3499446 demonstrates timedependent KRAS G12C protein target occupancy with IC50 of 24.2 nM at 5 minutes and a measured kinact/KI of 47,586 M-1sec-1.
TIME-DEPENDENT INHIBITION
IC50
|
||
|
INHIBITOR -> TARGET |
IN-VITRO
|
||
|
INHIBITOR -> TARGET |
Approved to target KRAS G12C mutations in the second-line setting,
|
||
|
|
INHIBITOR -> TARGET |
Selective for G12C mutant. Approved to target KRAS G12C mutations in the second-line setting.
IRREVERSIBLE INHIBITOR
IC50
|
||
|
|
INHIBITOR -> TARGET |
Picomolar cellular inhibition
IRREVERSIBLE INHIBITOR
IC50
|
||
|
INHIBITOR -> TARGET |
D3S-001 achieved rapid and near complete (> 95%) KRAS G12C inhibition within 2 hours at 5 nM.
IRREVERSIBLE INHIBITOR
kinact/Ki
|
||
|
INHIBITOR -> TARGET |
Preferentially targets the inactive state of KRAS to prevent its reactivation by nucleotide exchange.
|
||
|
INHIBITOR -> TARGET |
IRREVERSIBLE INHIBITOR
IC50
|
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| MOL_WEIGHT:NUMBER(CALCULATED) | CHEMICAL |
|
||||
| Molecular Formula | CHEMICAL |
|