Table 2.

Notum inhibition, MLM stability and MDCK-MDR1 cell permeability of thieno[2,3-d]pyrimidine amides 5.^a

NR1R2	Compound	Notum IC50 (nM)	MLM Cli (μL/min/mg)	MDCK-MDR1 AB/BA Papp (×10−6 cm/s) and efflux ratio (ER)
	5g	6.2 ± 0.5	33	23/62	2.7
	5h	4.2 ± 0.4	100	1.1/37	34
	5i	33 ± 5
	5j	450 ± 200
	5k	20 ± 4	63	7/51	7.3
	5l	2.4 ± 0.4	25	36/42	1.2
	5m	2.6 ± 0.1	43	35/51	1.5
	5n	3.8 ± 1.3	49
	5o	3.9 ± 0.4	140
	5p	16 ± 2	15	0.5/51	>100
	5q	23 ± 5	38	0.8/65	81
	5r	27 ± 3	53	0.8/78	97
	5s	38 ± 3	93	15/85	5.7
	5t	15 ± 3	53	19/49	2.6
	5u	11 ± 6	37	17/44	2.6
	5v	18 ± 5	140	15/27	1.8

^aSee footnotes Table 1.