Small molecule that mimics the binding of anti-EPPIN antibodies to EPPIN to provide male contraception, wherein the small molecule has one of the following formulas: and tautomers, and pharmaceutically-acceptable salts thereof, wherein: R 1 is -CH 2 R 5, R 2 is H, C 1-8 alkyl, C 1-8 haloalkyl, C 2-8 alkenyl, C 2-8 alkynyl, aryl, arylalkyl, alkylaryl, C R 6 or C XR 6, R 3 is -NHR 7, -C NHR 7, -NHC R 7, -NHC XR 7, -R 8, or -C R 8; R 4 is OR 7 or -C OR 7, R 5 is H, F, C 1-8 alkyl, C 1-8 haloalkyl, C 2-8 alkenyl, C 2-8 alkynyl, aryl, arylalkyl, alkylaryl, -XC XR 6, C XR 6, or C R 6, R 6 and R 7 are H, C 1-8 alkyl, C 1-8 haloalkyl, C 2-8 alkenyl, C 2-8 alkynyl, aryl, arylalkyl, or alkylaryl; R 8 is X is O, S, or NR 7, Y is O, S, NR 7, or C(R 7) 2, Zj refers to j number of Z substituents, which substituents can be present at any carbon atom on the benzene ring, wherein j is 0, 1 or 2, each Z is, individually, a substituent species selected from the group consisting of C 1-8 alkyl, C 1-8 substituted alkyl, C 2-8 alkenyl, C- 2-8 substituted alkenyl, heterocyclyl, substituted heterocyclyl, C 3-8 cycloalkyl, C 3-8 substituted cycloalkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, arylalkyl, substituted arylalkyl, halo, -OR 7, -N(R 7) 2, -CF 3, -CN, -NO 2, -C 2 R 7, -SR 7, -N 3, -C(=O)N(R 7) 2,-NR 7 C(=O)R 7, -C(=O)R 7, -C(=O)OR 7, -OC(=O)R 7, -O(CR 6 R 7) r C(=O)R 7 -,-O(CR 6 R 7) r NR 7 C(=O)R 7, -O(CR 6 R 7) r NR 7 SO 2 R 7, -OC(=O)NR 6 R 7,-NR 7 C(=O)OR 7, -SO 2 R 7,-SO 2 NR 6 R 7, and -NR 7 SO 2 R 7, r is an integer from 1 to 6, and n is 0, 1, 2, or 3, the term "substituted" as applied to alkyl, aryl, cycloalkyl refers to the substituents described above, starting with halo and ending with -NR 7 SO 2 R 7; and tautomers, and pharmaceutically-acceptable salts thereof, wherein the compounds can exist as single stereoisomers or as mixtures of stereoisomers,-optionally wherein haloalkyl is mono-fluoromethyl, R 5 is F, -XC XR 6, or C XR 6, or one or more C=X moieties are carbonyl (C=O). R 1 is -CH 2 R 5, R 2 is H, C 1-8 alkyl, C 1-8 haloalkyl, C 2-8 alkenyl, C 2-8 alkynyl, aryl, arylalkyl, alkylaryl, C R 6 or C XR 6, R 3 is -NHR 7, -C NHR 7, -NHC R 7, -NHC XR 7, -R 8, or -C R 8; R 4 is OR 7 or -C OR 7, R 5 is H, F, C 1-8 alkyl, C 1-8 haloalkyl, C 2-8 alkenyl, C 2-8 alkynyl, aryl, arylalkyl, alkylaryl, -XC XR 6, C XR 6, or C R 6, R 6 and R 7 are H, C 1-8 alkyl, C 1-8 haloalkyl, C 2-8 alkenyl, C 2-8 alkynyl, aryl, arylalkyl, or alkylaryl; R 8 is X is O, S, or NR 7, Y is O, S, NR 7, or C(R 7) 2, Zj refers to j number of Z substituents, which substituents can be present at any carbon atom on the benzene ring, wherein j is 0, 1 or 2, each Z is, individually, a substituent species selected from the group consisting of C 1-8 alkyl, C 1-8 substituted alkyl, C 2-8 alkenyl, C- 2-8 substituted alkenyl, heterocyclyl, substituted heterocyclyl, C 3-8 cycloalkyl, C 3-8 substituted cycloalkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, arylalkyl, substituted arylalkyl, halo, -OR 7, -N(R 7) 2, -CF 3, -CN, -NO 2, -C 2 R 7, -SR 7, -N 3, -C(=O)N(R 7) 2,-NR 7 C(=O)R 7, -C(=O)R 7, -C(=O)OR 7, -OC(=O)R 7, -O(CR 6 R 7) r C(=O)R 7 -,-O(CR 6 R 7) r NR 7 C(=O)R 7, -O(CR 6 R 7) r NR 7 SO 2 R 7, -OC(=O)NR 6 R 7,-NR 7 C(=O)OR 7, -SO 2 R 7,-SO 2 NR 6 R 7, and -NR 7 SO 2 R 7, r is an integer from 1 to 6, and n is 0, 1, 2, or 3, the term "substituted" as applied to alkyl, aryl, cycloalkyl refers to the substituents described above, starting with halo and ending with -NR 7 SO 2 R 7; and tautomers, and pharmaceutically-acceptable salts thereof, wherein the compounds can exist as single stereoisomers or as mixtures of stereoisomers,-optionally wherein haloalkyl is mono-fluoromethyl, R 5 is F, -XC XR 6, or C XR 6, or one or more C=X moieties are carbonyl (C=O).