Payload Information

General Information of This Payload

Payload ID	PAY0NBSXR
Name	GRM cpd 16
Synonyms	GRM cpd 16 Click to Show/Hide
Target(s)	Glucocorticoid receptor (NR3C1)			Target Info
Structure
Structure	3D MOL		2D MOL
Formula	C34H35F2NO6
Isosmiles	CC12C=CC(=O)C=C1C(F)CC1C3CC4OC(c5ccc(Cc6ccc(N)cc6)cc5)OC4(C(=O)CO)C3CC(O)C12F
InChI	InChI=1S/C34H35F2NO6/c1-32-11-10-22(39)13-26(32)27(35)15-25-23-14-30-33(29(41)17-38,24(23)16-28(40)34(25,32)36)43-31(42-30)20-6-2-18(3-7-20)12-19-4-8-21(37)9-5-19/h2-11,13,23-25,27-28,30-31,38,40H,12,14-17,37H2,1H3
InChIKey	PIPCZJIBKDNJLH-UHFFFAOYSA-N
Pharmaceutical Properties	Molecule Weight	591.651	Polar area	119.08
	Complexity	43	xlogp Value	4.1124
	Heavy Count	43	Rot Bonds	5
	Hbond acc	7	Hbond Donor	3

The activity data of This Payload

Standard Type	Value	Units	Cell line	Disease Model	Cell line ID	Reference
Glucocorticoid Receptor binding IC50	0.010±0.009	uM	Undisclosed	Undisclosed	Undisclosed	[1]
Glucocorticoid response element reporter EC50	0.0152±0.0126	uM	Undisclosed	Undisclosed	Undisclosed	[1]

Each Antibody-drug Conjugate Related to This Payload

Full Information of The Activity Data of The ADC(s) Related to This Payload

Anti-TNF ADC 105 [Investigative]

ADC Info

Revealed Based on the Cell Line Data

Click To Hide/Show 2 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2.18 ug/mL	Positive TNF expression (TNF+++/++)
Method Description	All the DAR purified ADCs were screened in both the TNF-expressing and wild-type K562 GRE reporter cell assay to confirm that their activity was consistent with ADCs having heterogeneous average DAR.
In Vitro Model	Chronic myelogenous leukemia	K-562 cells (TNF expression)		CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 50.00 ug/mL	Negative TNF expression (TNF-)
Method Description	All the DAR purified ADCs were screened in both the TNF-expressing and wild-type K562 GRE reporter cell assay to confirm that their activity was consistent with ADCs having heterogeneous average DAR.
In Vitro Model	Chronic myelogenous leukemia	K-562 cells		CVCL_0004

References

Ref 1	Discovery of ABBV-3373, an Anti-TNF Glucocorticoid Receptor Modulator Immunology Antibody Drug Conjugate. J Med Chem. 2022 Dec 8;65(23):15893-15934.
Ref 2	Discovery of ABBV-3373, an Anti-TNF Glucocorticoid Receptor Modulator Immunology Antibody Drug Conjugate. J Med Chem. 2022 Dec 8;65(23):15893-15934.