Payload Information

General Information of This Payload

Payload ID	PAY0XXLHN
Name	GRM cpd 19
Synonyms	GRM cpd 19 Click to Show/Hide
Target(s)	Glucocorticoid receptor (NR3C1)			Target Info
Structure
Structure	3D MOL		2D MOL
Formula	C34H36FNO6
Isosmiles	CC12C=CC(=O)C=C1CCC1C3CC4OC(c5ccc(Cc6cccc(N)c6)cc5)OC4(C(=O)CO)C3CC(O)C12F
InChI	InChI=1S/C34H36FNO6/c1-32-12-11-24(38)15-22(32)9-10-26-25-16-30-33(29(40)18-37,27(25)17-28(39)34(26,32)35)42-31(41-30)21-7-5-19(6-8-21)13-20-3-2-4-23(36)14-20/h2-8,11-12,14-15,25-28,30-31,37,39H,9-10,13,16-18,36H2,1H3
InChIKey	MHTDPERYDOMEJK-UHFFFAOYSA-N
Pharmaceutical Properties	Molecule Weight	573.661	Polar area	119.08
	Complexity	42	xlogp Value	4.1644
	Heavy Count	42	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 response element reporter EC50	0.0004	uM	Undisclosed	Undisclosed	Undisclosed	[1]
Glucocorticoid Receptor binding IC50	0.012	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 124 [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)	0.03 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

Anti-TNF ADC 123 [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)	0.03 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

Anti-TNF ADC 108 [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)	0.16 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)	4.70 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.