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Compound Detail

CHEMBL5287923

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COc1cc2nc(C)nc(N[C@H](C)c3cc(N)cc(C(F)(F)F)c3)c2cc1C1CCN(C(=O)CCCCCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](C)c2ccc(-c3scnc3C)cc2)C(C)(C)C)CC1

Basic Information

ChEMBL ID CHEMBL5287923
Phase Preclinical
Structure Type MOL
InChI Key IIUMLDLNPGCAPX-GGCSJQPYSA-N
11
Targets
30
Activities
3
Assay Types
4
PK Parameters
19
Publications
0
Known Names

Molecular Properties

1028.3
MW (Da)

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C54H68F3N9O6S
MW 1028.26

Activity Summary

EC50 19 meas. best 8.07
IC50 9 meas. best 8.16
Kd 2 meas. best 8.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CAL-62
CHEMBL1075413
IC50 8.16 8.16 7.0 1
NCI-H460
CHEMBL396
IC50 8.16 8.16 7.0 1
ASPC1
CHEMBL612588
IC50 8.16 8.16 7.0 1
Son of sevenless homolog 1
CHEMBL2079846
Kd 8.09 7.56 8.1 2
von Hippel-Lindau disease tumor suppressor/SOS1
CHEMBL5169070
EC50 8.07 7.9911 8.4 19
MIA PaCa-2
CHEMBL614725
IC50 8.0 8.0 10.1 1
NCI-H358
CHEMBL614135
IC50 7.89 7.89 12.9 1
PANC-1
CHEMBL614139
IC50 7.86 7.86 13.8 1
SW-620
CHEMBL612262
IC50 7.73 7.73 18.5 1
LoVo
CHEMBL614721
IC50 7.35 7.35 44.5 1
A549
CHEMBL392
IC50 6.98 6.98 105.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 14090.0 ng.hr.mL-1 Mus musculus
AUC 14090.0 ng.hr.mL-1 Mus musculus
T1/2 9.69 hr Mus musculus
T1/2 9.69 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
CAL-62 IC50 = 6.97 nM 8.16 Antiproliferative activity against human CAL-62 cells harboring KRAS G12R mutant... 37778239
NCI-H460 IC50 = 6.97 nM 8.16 Antiproliferative activity against human NCI-H460 cells harboring KRAS Q16H muta... 37778239
ASPC1 IC50 = 6.97 nM 8.16 Antiproliferative activity against human ASPC1 cells harboring KRAS G12D mutant ... 36897932
Son of sevenless homolog 1 Kd = 8.13 nM 8.09 Binding affinity to GST-tagged human SOS1 (564 to 1049 residues) expressed in Es... 36897932
von Hippel-Lindau disease tumor suppressor/SOS1 EC50 = 8.41 nM 8.07 PROTAC activity at VHL/SOS1 in human Calu-1 cells harboring KRAS G12C mutant ass... 36897932
von Hippel-Lindau disease tumor suppressor/SOS1 EC50 = 8.41 nM 8.07 PROTAC activity at VHL/SOS1 in human Lovo cells harboring KRAS G13D mutant asses... 36897932
von Hippel-Lindau disease tumor suppressor/SOS1 EC50 = 8.41 nM 8.07 PROTAC activity at VHL/SOS1 in human HCT-116 cells harboring KRAS G13D mutant as... 36897932
von Hippel-Lindau disease tumor suppressor/SOS1 EC50 = 8.41 nM 8.07 PROTAC activity at VHL/SOS1 in human A549 cells harboring KRAS G12S mutant asses... 36897932
von Hippel-Lindau disease tumor suppressor/SOS1 EC50 = 8.41 nM 8.07 PROTAC activity at VHL/SOS1 in human NCI-H441 cells harboring KRAS G12V mutant a... 36897932
von Hippel-Lindau disease tumor suppressor/SOS1 EC50 = 8.41 nM 8.07 PROTAC activity at VHL/SOS1 in human SW620 cells harboring KRAS G12V mutant asse... 36897932
von Hippel-Lindau disease tumor suppressor/SOS1 EC50 = 8.41 nM 8.07 PROTAC activity at VHL/SOS1 in human SW480 cells harboring KRAS G12V mutant asse... 36897932
von Hippel-Lindau disease tumor suppressor/SOS1 EC50 = 8.41 nM 8.07 PROTAC activity at VHL/SOS1 in human MIA PaCa-2 cells harboring KRAS G12C mutant... 36897932
von Hippel-Lindau disease tumor suppressor/SOS1 EC50 = 8.41 nM 8.07 PROTAC activity at VHL/SOS1 in human UMUC3 cells harboring KRAS G12C mutant asse... 36897932
von Hippel-Lindau disease tumor suppressor/SOS1 EC50 = 8.41 nM 8.07 PROTAC activity at VHL/SOS1 in human SNU-C2B cells harboring KRAS G12D mutant as... 36897932
von Hippel-Lindau disease tumor suppressor/SOS1 EC50 = 8.41 nM 8.07 PROTAC activity at VHL/SOS1 in human ASPC1 cells harboring KRAS G12D mutant asse... 36897932
von Hippel-Lindau disease tumor suppressor/SOS1 EC50 = 8.41 nM 8.07 PROTAC activity at VHL/SOS1 in human HPAF-II cells harboring KRAS G12D mutant as... 36897932
von Hippel-Lindau disease tumor suppressor/SOS1 EC50 = 8.41 nM 8.07 PROTAC activity at VHL/SOS1 in human PANC-1 cells harboring KRAS G12D mutant ass... 36897932
von Hippel-Lindau disease tumor suppressor/SOS1 EC50 = 8.41 nM 8.07 PROTAC activity at VHL/SOS1 in human SK-LU-1 cells harboring KRAS G12D mutant as... 36897932
von Hippel-Lindau disease tumor suppressor/SOS1 EC50 = 8.41 nM 8.07 PROTAC activity at VHL/SOS1 in human SNU1 cells harboring KRAS G12D mutant asses... 36897932
von Hippel-Lindau disease tumor suppressor/SOS1 EC50 = 8.41 nM 8.07 PROTAC activity at VHL/SOS1 in human SK-CO-1 cells harboring KRAS G12V mutant as... 36897932

Literature References

Data from ChEMBL 36 via Core Engine