Table 1. Biochemical and biological activities of hits.

	KD or Ki (µM)			% pGAB1 inhibition	IC50 (µM)
ID	GAB1	IRS1	AKT1		MDA-MB-231	T47D
GAB-001	9.38±1.60*	NB	ND	55	40.3±1.3	23.7±2.7
GAB-002	2.1±0.1	16.4±4.3	ND	32	142.7±11.6	137.6±6.9
GAB-003	2.7±0.8	3.3±1.5	ND	14	85.2±7.2	13.9±0.6
GAB-004	2.2±1.1	NB	ND	81	66.6±4.6	19.4±2.9
GAB-005	NB	NB	ND	6	IA	IA
GAB-006	NB	NB	ND	16	ND	100.8±1.8
GAB-007	42.3±8.9	1.6±0.2	ND	53	4.6±0.7	20.1±4.3
GAB-008	NB	16.2±1.7	ND	8	IA	43.2±3.2
GAB-009	NB	NB	ND	38	162.9±6.0	97.6±6.1
GAB-010	NB	0.12±0.02	ND	92	66.0±4.4	23.8±4.2
GAB-011	NB	NB	ND	24	IA	IA
GAB-012	NB	NB	4.58±1.72	43	IA	119.2±3.6
GAB-013	NB	NB	6.27±1.16	27	IA	IA
GAB-014	NB	NB	NB	42	69.9±0.1**	177.5±3.9
GAB-015	13.1±1.5*	0.05	5.0±0.4*	77	71.7±1.6	125.4±5.4
GAB-016	0.9±0.1	0.15	4.3±0.1*	96	79.0±1.1	45.9±1.6
GAB-017	0.68±0.03	0.05	18.9±1.2*	82	40.6±0.8	41.4±2.7
GAB-018	36.6±5.0*	NB	6.0±1.0*	71	85.3±1.5	185.4±2.5
GAB-019	ND	ND	ND	91	ND	39.4±6.2
GAB-020	1.33±4.5	ND	2.4±0.6*	87	ND	68.2±5.5
DPIEL	2.8	ND	5.04±0.48	72	ND	30.6±4.3
IP4	ND	ND	3.08±0.49	ND	ND	ND

*Ki measurement.

**MDA-MB-468 cell line used.

ND: Not Determined. NB: No Binding. IA: Inactive.