Payload ID	PAY0ZHKZT
Name	(S)B19
Synonyms	(S)B19    Click to Show/Hide
Target	Eukaryotic peptide chain release factor GTP-binding subunit ERF3A (GSPT1)					Target Info
Structure
	3D MOL			2D MOL
Formula	C29H34ClN5O5
Isosmiles	O=C1C(C=CC(CNC(NC(C=C2)=CC(Cl)=C2CCCO[C@@H]3CNCCC3)=O)=C4)=C4CN1C(CCC5=O)C(N5)=O
InChI	InChI=1S/C29H34ClN5O5/c30-24-14-21(7-6-19(24)3-2-12-40-22-4-1-11-31-16-22)33-29(39)32-15-18-5-8-23-20(13-18)17-35(28(23)38)25-9-10-26(36)34-27(25)37/h5-8,13-14,22,25,31H,1-4,9-12,15-17H2,(H2,32,33,39)(H,34,36,37)/t22-,25?/m0/s1
InChIKey	AUCAGMGHZBLJIS-XADRRFQNSA-N
Pharmaceutical Properties	Molecule Weight		568.074	Polar area		128.87
	Complexity		1246.794577	xlogp Value		3.1239
	Heavy Count		40	Rot Bonds		9
	Hbond acc		6	Hbond Donor		4

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	63%	High CD123 expression (CD123+++)
Method Description	Investigated the antitumour effect of 5mg/kg ADC in a CD33highCD123high MV-4-11 xenograft NOD SCID mice tumour model, D19.
In Vivo Model	CD123-high MV-4-11 xenograft NOD SCID mice tumour model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.2666 pM	High CD33 expression (CD33+++)
Method Description	Cytotoxicity of ADC to MV4-11 cells
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	65%	Low HER2 expression (HER2+)
Method Description	Investigated the antitumour effect of 3mg/kg T-ADC in a HER2low JIMT-1 xenograft NUNU mice tumour model, D26.
In Vivo Model	HER2-low JIMT-1 xenograft NUNU mice tumour model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	88%	High HER2 expression (HER2+++)
Method Description	Investigated the antitumour effect of 3mg/kg ADC in a HER2high HCC-1954 xenograft NUNU mice tumour model, D21.
In Vivo Model	HER2-high HCC-1954 xenograft NUNU mice tumour model
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	95%	Low HER2 expression (HER2+)
Method Description	Investigated the antitumour effect of 5mg/kg ADC in a HER2low JIMT-1 xenograft NUNU mice tumour model, D13.
In Vivo Model	HER2-low JIMT-1 xenograft NUNU mice tumour model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.8 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to BT-474 cells
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 25 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.01676 nM	Low HER2 expression (HER2+)
Method Description	Cytotoxicity of ADC to T-47D cells
In Vitro Model	Invasive breast carcinoma of no special type	T-47D cells		CVCL_0553
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.4645 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to NCI-N87 cells
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	90.10%	Low HER2 expression (HER2+)
Method Description	Investigated the antitumour effect of 5mg/kg ADC in a HER2low JIMT-1 xenograft NUNU mice tumour model, D13.
In Vivo Model	HER2-low JIMT-1 xenograft NUNU mice tumour model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 15 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	100.20%	High CD33 expression (CD33+++)
Method Description	Investigated the antitumour effect of 0.1 mg/kg ADC in a CD33highCD123high MV-4-11 xenograft NOD SCID mice tumour model, D14.
In Vivo Model	CD123-high MV-4-11 xenograft NOD SCID mice tumour model
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	108.60%	High CD33 expression (CD33+++)
Method Description	Investigated the antitumour effect of 1mg/kg ADC in a CD33high MV-4-11 xenograft NOD SCID mice tumour model, D19.
In Vivo Model	CD33-high MV-4-11 xenograft NOD SCID mice tumour model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.475 pM	High CD33 expression (CD33+++)
Method Description	Cytotoxicity of ADC to MV4-11 cells
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	108.30%	High CD33 expression (CD33+++)
Method Description	Investigated the antitumour effect of 1mg/kg ADC in a CD33high MV-4-11 xenograft NOD SCID mice tumour model, D19.
In Vivo Model	CD33-high MV-4-11 xenograft NOD SCID mice tumour model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.486 pM	High CD33 expression (CD33+++)
Method Description	Cytotoxicity of ADC to MV4-11 cells
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	108.70%	High CD33 expression (CD33+++)
Method Description	Investigated the antitumour effect of 1mg/kg ADC in a CD33high MV-4-11 xenograft NOD SCID mice tumour model, D19.
In Vivo Model	CD33-high MV-4-11 xenograft NOD SCID mice tumour model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	5.355 pM	High CD33 expression (CD33+++)
Method Description	Cytotoxicity of ADC to MV4-11 cells
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.404 pM	High CD33 expression (CD33+++)
Method Description	Cytotoxicity of ADC to MV4-11 cells
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	12.3 pM	High CD33 expression (CD33+++)
Method Description	Cytotoxicity of ADC to MV4-11 cells
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 15 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	15-25 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	15-25 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 15 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	15-25 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 25 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.12 nM	High BCMA expression (BCMA+++)
Method Description	Cytotoxicity of ADC to NCI-H929 cells
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.14 nM	High BCMA expression (BCMA+++)
Method Description	Cytotoxicity of ADC to NCI-H929 cells
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.21 nM	High BCMA expression (BCMA+++)
Method Description	Cytotoxicity of ADC to NCI-H929 cells
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.29 nM	High BCMA expression (BCMA+++)
Method Description	Cytotoxicity of ADC to NCI-H929 cells
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600

Ref 1	Antibody-drug conjugate