Payload Information
General Information of This Payload
| Payload ID | PAY0CGHRL |
|||||
|---|---|---|---|---|---|---|
| Name | MK4827 |
|||||
| Synonyms |
MK4827
Click to Show/Hide
|
|||||
| Structure |
|
|||||
| Formula | C19H20N4O |
|||||
| Isosmiles | O=C(N)C1=CC=CC(C1=N2)=CN2C3=CC=C([C@H]4CNCCC4)C=C3 |
|||||
| PubChem CID | ||||||
| InChI |
InChI=1S/C19H20N4O/c20-19(24)17-5-1-3-15-12-23(22-18(15)17)16-8-6-13(7-9-16)14-4-2-10-21-11-14/h1,3,5-9,12,14,21H,2,4,10-11H2,(H2,20,24)/t14-/m1/s1
|
|||||
| InChIKey |
PCHKPVIQAHNQLW-CQSZACIVSA-N
|
|||||
| Pharmaceutical Properties | Molecule Weight |
320.396 |
Polar area |
72.94 |
||
Complexity |
854.694631 |
xlogp Value |
2.5914 |
|||
Heavy Count |
24 |
Rot Bonds |
3 |
|||
Hbond acc |
4 |
Hbond Donor |
2 |
|||
The activity data of This Payload
| Standard Type | Value | Units | Cell line | Disease Model | Cell line ID | Reference |
|---|---|---|---|---|---|---|
| Cell-based Percent Inhibition (%) | -28.65 | % | Undisclosed | Undisclosed | Undisclosed | |
| Cell-based Percent Inhibition (%) | 0.2 | % |
Vero C1008 cells
|
Normal
|
||
| Cell-based Percent Inhibition (%) | 0.2 | % |
Vero C1008 cells
|
Normal
|
||
| Cell-based Percent Inhibition (%) | 0.21 | % |
Vero C1008 cells
|
Normal
|
||
| Cell-based Percent Inhibition (%) | 0.21 | % |
Vero C1008 cells
|
Normal
|
||
| Cell-based Percent Inhibition (%) | <10 | % |
CAPAN-1 cells
|
Pancreatic ductal adenocarcinoma
|
||
| Cell-based Percent Inhibition (%) | 10 | % | Undisclosed | Undisclosed | Undisclosed | |
| Cell-based Percent Inhibition (%) | 2.32 | % |
Caco-2 cells
|
Colon adenocarcinoma
|
||
| Cell-based Percent Inhibition (%) | 31.76 | % | Undisclosed | Undisclosed | Undisclosed | |
| Cell-based Percent Inhibition (%) | 42.76 | % | Undisclosed | Undisclosed | Undisclosed | |
| Cell-based Percent Inhibition (%) | >50 | % | Undisclosed | Undisclosed | Undisclosed | |
| Cell-based Percent Inhibition (%) | >50 | % | Undisclosed | Undisclosed | Undisclosed | |
| Tumor Growth Inhibition (TGI) | 57.24 | % |
MDA-MB-231 cells
|
Breast adenocarcinoma
|
||
| Tumor Growth Inhibition (TGI) | 60 | % |
CAPAN-1 cells
|
Pancreatic ductal adenocarcinoma
|
||
| Cell-based Percent Inhibition (%) | 9.09 | % | Undisclosed | Undisclosed | Undisclosed | |
| Cell-based Percent Inhibition (%) | >90 | % |
CAPAN-1 cells
|
Pancreatic ductal adenocarcinoma
|
||
| Cell-based Percent Inhibition (%) | >90 | % |
MDA-MB-436 cells
|
Metastasis of ductal carcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | >10000 | nM |
Sf9 cells
|
Normal
|
||
| Half Maximal Inhibitory Concentration (IC50) | >10000 | nM |
Sf9 cells
|
Normal
|
||
| Half Maximal Inhibitory Concentration (IC50) | >10000 | nM |
Sf9 cells
|
Normal
|
||
| Half Maximal Inhibitory Concentration (IC50) | >10000 | nM |
Sf9 cells
|
Normal
|
||
| Half Maximal Inhibitory Concentration (IC50) | >10000 | nM |
Sf9 cells
|
Normal
|
||
| Half Maximal Inhibitory Concentration (IC50) | >10000 | nM |
Sf9 cells
|
Normal
|
||
| Half Maximal Inhibitory Concentration (IC50) | >10000 | nM |
Sf9 cells
|
Normal
|
||
| Half Maximal Inhibitory Concentration (IC50) | >10000 | nM |
Sf9 cells
|
Normal
|
||
| Half Maximal Inhibitory Concentration (IC50) | >10000 | nM |
Sf9 cells
|
Normal
|
||
| Half Maximal Inhibitory Concentration (IC50) | >10000 | nM |
Sf9 cells
|
Normal
|
||
| Half Maximal Inhibitory Concentration (IC50) | 10000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | 1004 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 11070 | nM |
MDA-MB-231 cells
|
Breast adenocarcinoma
|
||
| Half Maximal Activity Concentration (AC50) | 113.1 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | 1173.2 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 11770 | nM |
MCF-7 cells
|
Invasive breast carcinoma of no special type
|
||
| Half Maximal Inhibitory Concentration (IC50) | 12550 | nM |
A549 cells
|
Lung adenocarcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 127 | nM |
HEC-1B cells
|
Endometrial adenocarcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 1300 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 131.83 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 132 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 13350 | nM |
MDA-MB-231 cells
|
Breast adenocarcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 1410 | nM |
MCF-7 cells
|
Invasive breast carcinoma of no special type
|
||
| Half Maximal Activity Concentration (AC50) | 14403.9 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 1443 | nM |
Sf9 cells
|
Normal
|
||
| Half Maximal Inhibitory Concentration (IC50) | 149 | nM |
DLD-1 cells
|
Colon adenocarcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 15.3 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 15.3 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 15.49 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | 15320 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 15360 | nM |
BT-549 cells
|
Breast ductal carcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 16.22 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 16.7 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 16.7 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 16.7 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 1690 | nM |
MV4-11 cells
|
Childhood acute monocytic leukemia
|
||
| Half Maximal Inhibitory Concentration (IC50) | 17300 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 1737.8 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 1800 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 1810 | nM |
HCT116 cells
|
Colon carcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 1900 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 1945 | nM |
Sf9 cells
|
Normal
|
||
| Half Maximal Inhibitory Concentration (IC50) | 1949.84 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 2 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 2.1 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 2.1 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 2.1 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 2.1 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Effective Concentration (EC50) | 200 | nM |
Jurkat cells
|
Childhood T acute lymphoblastic leukemia, Precursor T-cell acute lymphoblastic leukemia
|
||
| Half Maximal Inhibitory Concentration (IC50) | 21130 | nM |
NCM460 cells
|
Normal
|
||
| Half Maximal Inhibitory Concentration (IC50) | 22430 | nM |
BT-549 cells
|
Breast ductal carcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 2344.23 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 2355 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 24 | nM |
Ishikawa cells
|
Endometrial adenocarcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 254 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | 25999.8 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 28840.32 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 29200 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | 29390 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 295.12 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 296 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 297 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 3.2 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 3.5 | nM |
CAPAN-1 cells
|
Pancreatic ductal adenocarcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 3.8 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 3.8 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 3.8 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 3.8 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 3.8 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 30 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Activity Concentration (AC50) | >30000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Effective Concentration (EC50) | 31000 | nM |
Jurkat cells
|
Childhood T acute lymphoblastic leukemia, Precursor T-cell acute lymphoblastic leukemia
|
||
| Half Maximal Inhibitory Concentration (IC50) | 32.3 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 330 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 3300 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 3311.31 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 33220 | nM |
MDA-MB-231 cells
|
Breast adenocarcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 35 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 35 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 35000 | nM |
Cancer cells
|
Multiple myeloma, Plasma cell myeloma
|
Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 3820 | nM |
MV4-11 cells
|
Childhood acute monocytic leukemia
|
||
| Half Maximal Effective Concentration (EC50) | 4 | nM |
HeLa cells
|
Human papillomavirus-related endocervical adenocarcinoma
|
||
| Half Maximal Effective Concentration (EC50) | 4 | nM |
HeLa cells
|
Human papillomavirus-related endocervical adenocarcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 4 | nM |
A2780 cells
|
Ovarian endometrioid adenocarcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 4.67 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | >40000 | nM |
MCF-10A cells
|
Normal
|
||
| Half Maximal Inhibitory Concentration (IC50) | >40000 | nM |
MCF-10A cells
|
Normal
|
||
| Half Maximal Inhibitory Concentration (IC50) | >40000 | nM |
MCF-10A cells
|
Normal
|
||
| Half Maximal Inhibitory Concentration (IC50) | >40000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 4170 | nM |
A549 cells
|
Lung adenocarcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 446 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 446.68 | nM | Undisclosed | Undisclosed | Undisclosed | |
| 90% Effective Concentration (EC90) | 45 | nM |
HeLa cells
|
Human papillomavirus-related endocervical adenocarcinoma
|
||
| 90% Inhibitory Concentration (IC90) | 46 | nM |
HeLa cells
|
Human papillomavirus-related endocervical adenocarcinoma
|
||
| 90% Inhibitory Concentration (IC90) | 50 | nM |
CAPAN-1 cells
|
Pancreatic ductal adenocarcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 5128.61 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 5130 | nM | Undisclosed | Undisclosed | Undisclosed | |
| 90% Inhibitory Concentration (IC90) | 52 | nM |
A2780 cells
|
Ovarian endometrioid adenocarcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 53710 | nM |
NCM460 cells
|
Normal
|
||
| Half Maximal Inhibitory Concentration (IC50) | 570 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 60910 | nM |
MDA-MB-231 cells
|
Breast adenocarcinoma
|
||
| Half Maximal Effective Concentration (EC50) | 620.8 | nM |
CAPAN-1 cells
|
Pancreatic ductal adenocarcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 6320 | nM |
MDA-MB-231 cells
|
Breast adenocarcinoma
|
||
| Half Maximal Effective Concentration (EC50) | 650 | nM |
CAPAN-1 cells
|
Pancreatic ductal adenocarcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 7600 | nM |
MDA-MB-468 cells
|
Breast adenocarcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 79 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 794.33 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 8.05 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 800 | nM |
MCF-7 cells
|
Invasive breast carcinoma of no special type
|
||
| Half Maximal Inhibitory Concentration (IC50) | 8280 | nM |
BT-549 cells
|
Breast ductal carcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 830 | nM |
HCT116 cells
|
Colon carcinoma
|
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
YC1667 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
5.623 ng/mL
|
Positive PSMA expression (PSMA+++/++) | ||
| Method Description |
ADCs (10x the final top concentration) was tested in C4-2B cells for 3 days.
|
||||
| In Vitro Model | Prostate carcinoma | LNCaP cells | CVCL_0395 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
11.16 ng/mL
|
Positive PSMA expression (PSMA+++/++) | ||
| Method Description |
ADCs (10x the final top concentration) was tested in LNCap cells for 3 days.
|
||||
| In Vitro Model | Prostate carcinoma | LNCaP cells | CVCL_0395 | ||