Table 3.

Aminobenzimidazole-based mIDH1-inhibitors listed by decreasing potency.

R1	R2	R3	R4	R5	IC50 a
	OMe			H	3 nm
	H			H	4 nm
	Me			H	4 nm
	Cl			H	6 nm
	OMe			H	6 nm
	Me			H	7 nm
	OMe			H	8 nm
	H			F	9 nm
	OMe			H	9 nm
	OMe			H	9 nm
	H			H	10 nm
H	OEt			H	10 nm
	H			H	15 nm b
	Me			H	20 nm
	OMe			H	20 nm
	Me			H	20 nm
	H			F	20 nm
	Me			H	20 nm
	H			H	20 nm
	OMe			H	20 nm
	F			H	20 nm
H	Me			H	20 nm
				H	20 nm
H	Me			F	20 nm
	OMe			H	30 nm
	Me			H	30 nm
	Me			H	30 nm
	H			F	30 nm
H	H			H	30 nm
	H			H	30 nm
	Cl			H	30 nm
	H			H	30 nm
	OMe			H	30 nm
OMe	H			H	30 nm
	Cl			H	30 nm
	Me			H	30 nm
				H	30 nm
H	H			OMe	30 nm
H	Me			Me	40 nm
	H			H	40 nm
	Me			H	40 nm
	H			H	40 nm
H	OEt			H	40 nm
H	OMe			H	40 nm
	H			H	50 nm
	H			H	50 nm
	Cl			H	60 nm
	Me			H	60 nm
H	OMe			H	60 nm
	H			OMe	70 nm
	H			OMe	70 nm
H	H			H	70 nm
H	H			F	70 nm
H	H			F	70 nm
	H			H	70 nm
	OMe			H	70 nm
H2N	H			H	70 nm
	H			OMe	70 nm
OMe	H			H	70 nm
H	Me			F	70 nm
H2N	H			H	80 nm
CN	H			H	80 nm
CN	Me			H	80 nm
	OMe			H	80 nm
H	H			OMe	80 nm
	H			H	90 nm
	H			Me	90 nm
	Cl			H	90 nm
	Cl			H	90 nm
	OMe			H	90 nm
	H			H	90 nm
	H			OMe	100 nm

^a IC₅₀ values for biochemical assays with IDH1_R132H homodimers, compiled from [80,98]; ^b BAY1436032.