A compound of Formula: wherein R 1 is H; R 2 is selected from the group consisting of: CH 2 -cyclohexyl, wherein the cyclohexyl is optionally substituted with OH; 3-hydroxyadamantan-1-yl; and C 3-6 cycloalkyl optionally substituted with 1, 2, or 3 substituents each independently selected from the group consisting of: OH, halogen, C 1-6 alkyl, C 1-6 haloalkyl, OC 1-6 alkyl, CN, NR 6 R 7, NR 8 -C H, NR 8 -C -C 1-6 alkyl, NR 8 -C -C 1-6 haloalkyl, NR 8 -C -O-C 1-6 alkyl, NR 8 -C -C 1-6 alk-OH, NR 8 -C -C 1-6 alk-NR 6 R 7, and NR 8 -C -C(R 3)=CR 4 (R 5); wherein R 3 is selected from the group consisting of: H, CN, halogen, C 1-6 haloalkyl, and C 1-6 alkyl; R 4 and R 5 are each independently selected from the group consisting of: H; C 0-6 alk-NR 6 R 7; C 1-6 alk-O-C 1-6 alkyl; C 3-6 cycloalkyl; heterocycloalkyl optionally substituted with C 1-6 alkyl; and -linker-PEG- Biotin; R 6 and R 7 are each independently selected from the group consisting of: H, C 1-6 alkyl, C H, and CN; and R 8 is H; or R 1 and R 2, together with the nitrogen atom to which they are attached, form a pyrrolidinyl ring optionally substituted with NR 6 R 7, wherein R 6 and R 7 are each independently selected from the group consisting of H; C 1-6 alkyl; NR 8 -C -C 1-6 alkyl; and NR 8 -C -C(R 3)=CR 4 (R 5), wherein R 3 is H or CN; R 4 is H; and R 5 is H or cyclopropyl; A is selected from the group consisting of: pyridyl; phenyl; pyrimidinyl; pyrazinyl; pyridin-2 -one; and pyridazinyl; wherein the A is optionally substituted with 1, 2, or 3 substituents each independently selected from the group consisting of: halogen, C 1-6 alkyl, C 1-6 haloalkyl, and OC 1-6 alkyl; E is selected from the group consisting of: O, a bond, and CH 2; G is selected from the group consisting of: H; halogen; C 1-6 alkyl; C 1-6 haloalkyl; NH(C 1-6 alkyl); C 3-6 cycloalkyl; phenyl; pyrimidinyl; pyridyl; pyridazinyl; pyridin-2 -one; heterocycloalkyl that contains an oxygen heteroatom; and phenyl-CH 2 -O-phenyl, wherein the -O-phenyl is substituted with CN; wherein the phenyl; pyridyl; pyridazinyl; and pyridin-2 -one is optionally substituted with 1, 2, or 3 substituents each independently selected from the group consisting of: halogen, C 1-6 alkyl, C 1-6 haloalkyl, OC 1-6 haloalkyl, and OC 1-6 alkyl; and stereoisomers and isotopic variants thereof; and pharmaceutically acceptable salts thereof. R 1 is H; R 2 is selected from the group consisting of: CH 2 -cyclohexyl, wherein the cyclohexyl is optionally substituted with OH; 3-hydroxyadamantan-1-yl; and C 3-6 cycloalkyl optionally substituted with 1, 2, or 3 substituents each independently selected from the group consisting of: OH, halogen, C 1-6 alkyl, C 1-6 haloalkyl, OC 1-6 alkyl, CN, NR 6 R 7, NR 8 -C H, NR 8 -C -C 1-6 alkyl, NR 8 -C -C 1-6 haloalkyl, NR 8 -C -O-C 1-6 alkyl, NR 8 -C -C 1-6 alk-OH, NR 8 -C -C 1-6 alk-NR 6 R 7, and NR 8 -C -C(R 3)=CR 4 (R 5); wherein R 3 is selected from the group consisting of: H, CN, halogen, C 1-6 haloalkyl, and C 1-6 alkyl; R 4 and R 5 are each independently selected from the group consisting of: H; C 0-6 alk-NR 6 R 7; C 1-6 alk-O-C 1-6 alkyl; C 3-6 cycloalkyl; heterocycloalkyl optionally substituted with C 1-6 alkyl; and -linker-PEG- Biotin; R 6 and R 7 are each independently selected from the group consisting of: H, C 1-6 alkyl, C H, and CN; and R 8 is H; R 3 is selected from the group consisting of: H, CN, halogen, C 1-6 haloalkyl, and C 1-6 alkyl; R 4 and R 5 are each independently selected from the group consisting of: H; C 0-6 alk-NR 6 R 7; C 1-6 alk-O-C 1-6 alkyl; C 3-6 cycloalkyl; heterocycloalkyl optionally substituted with C 1-6 alkyl; and -linker-PEG- Biotin; R 6 and R 7 are each independently selected from the group consisting of: H, C 1-6 alkyl, C H, and CN; and R 8 is H; H, C 1-6 alkyl, C H, and CN; and R 8 is H; or R 1 and R 2, together with the nitrogen atom to which they are attached, form a pyrrolidinyl ring optionally substituted with NR 6 R 7, wherein R 6 and R 7 are each independently selected from the group consisting of H; C 1-6 alkyl; NR 8 -C -C 1-6 alkyl; and NR 8 -C -C(R 3)=CR 4 (R 5), wherein R 3 is H or CN; R 4 is H; and R 5 is H or cyclopropyl; A is selected from the group consisting of: pyridyl; phenyl; pyrimidinyl; pyrazinyl; pyridin-2 -one; and pyridazinyl; wherein the A is optionally substituted with 1, 2, or 3 substituents each independently selected from the group consisting of: halogen, C 1-6 alkyl, C 1-6 haloalkyl, and OC 1-6 alkyl; E is selected from the group consisting of: O, a bond, and CH 2; G is selected from the group consisting of: H; halogen; C 1-6 alkyl; C 1-6 haloalkyl; NH(C 1-6 alkyl); C 3-6 cycloalkyl; phenyl; pyrimidinyl; pyridyl; pyridazinyl; pyridin-2 -one; heterocycloalkyl that contains an oxygen heteroatom; and phenyl-CH 2 -O-phenyl, wherein the -O-phenyl is substituted with CN; wherein the phenyl; pyridyl; pyridazinyl; and pyridin-2 -one is optionally substituted with 1, 2, or 3 substituents each independently selected from the group consisting of: halogen, C 1-6 alkyl, C 1-6 haloalkyl, OC 1-6 haloalkyl, and OC 1-6 alkyl; and stereoisomers and isotopic variants thereof; and pharmaceutically acceptable salts thereof. halogen, C 1-6 alkyl, C 1-6 haloalkyl, OC 1-6 haloalkyl, and OC 1-6 alkyl; and stereoisomers and isotopic variants thereof; and pharmaceutically acceptable salts thereof.