Chemogenomic set

Screened at 1 µM, closest targets as % of contr.: JNK2(4%), KIT(2%), PDGFRB(0%)

Screened at 10 µM, closest targets: IC50(MAPK15) = 130 nM, IC50(RPS6KA3) = 361 nM, IC50(RPS6KA2) = 362 nM; IC50(FLT3) = 582 nM, IC50(NUAK1) = 711 nM, IC50(CLK2) = 1370 nM (Z’-Lyte assay)

Screened at 10 µM, follow-up Kds and IC50s of closest targets: Kd(FLT1,D835Y) = 210 nM, Kd(CKL1) = 310 nM, Kd(MKNK2) = 330 nM, IC50(AKT3) = 427 nM.

Screened at 10 µM, follow-up Kds and IC50s of closest targets: Kd(FLT1,D835Y) = 210 nM, Kd(CKL1) = 310 nM, Kd(MKNK2) = 330 nM, IC50(AKT3) = 427 nM.

Screened at 1 µM, closest targets as % of contr.: ERBB2 (2.1%), ERBB4 (4.3%), TEC (6.4%); Inhibits kinases containing conserved cystein residue: IC50(BMX) = 46 nM, IC50(ERBB4) = 16 nM, IC50(TEC) = 93 nM, IC50(TXK) = 368 nM, IC50(ERBB2) = 1000 nM (Z’-LYTE assay), PMID: 26641137;

Screened at 200 nM, closest targets with >90% inhibition: IRAK1, targets with >70% inhibition: MNK2, LRRK2, CLK4, CK1g; Screened in KiNativ kinome screen (ActivX) in THP1 cell lysates at 10, 50, 200, 1000, and 5000 nM against 270 kinases; closest targets >50% inhibition at 200 nM: CSNK1G2, IRAK3, PIPK2C, CKSNK1D/E, https://pubmed.ncbi.nlm.nih.gov/28498658/; Cellular potency (NanoBRET assay in HEK293T cells): IC50(CSNK1G2) = 7.1 µM (SGC-Frankfurt, in-house data)

Screened at 1 µM, closest targets as % of contr.: BMX (15%), ROS1 (12%), TXK (14%), TNK2(10%)

Screened at 1 µM, closest targets as % of contr.: BMX (15%), ROS1 (12%), TXK (14%), TNK2(10%)

Screened at 1 µM, closest targets as % of contr.: BMX (15%), ROS1 (12%), TXK (14%), TNK2(10%)

Screened at 3 µM, closest targets as % inhibition: CLK1 (99%), DYRK1A/B (94/98%), DYRK3 (95%), PHKG (96%); In vitro follow-up (Invitrogen): IC50(DYRK3) = 99 nM, IC50(DYRK1A/B) = 104/157 nM, IC50(PHKG) = 136 nM, IC50(CLK3) = 300 nM; Cellular selectivity: IC50(JNK1/2/3) = 0.68 µM, IC50(CAMKK2) = 1.10 µM, IC50(PIP4K2C) = 1.30 µM (ActivX KiNative profiling assay (in HCT-116 cell line (CRL-1619))

Screened at 3 µM, closest targets as % inhibition: CLK1 (99%), DYRK1A/B (94/98%), DYRK3 (95%), PHKG (96%); In vitro follow-up (Invitrogen): IC50(DYRK3) = 99 nM, IC50(DYRK1A/B) = 104/157 nM, IC50(PHKG) = 136 nM, IC50(CLK3) = 300 nM; Cellular selectivity: IC50(JNK1/2/3) = 0.68 µM, IC50(CAMKK2) = 1.10 µM, IC50(PIP4K2C) = 1.30 µM (ActivX KiNative profiling assay (in HCT-116 cell line (CRL-1619))

Closest target: AKT3 (83% of ctrl.); Follow up in vitro activity: IC50(AKT3) = 618 nM (HTFR assay, PMID: 31584233), IC50(AKT3) = 4.3 µM (NanoBRET assay)

Closest target: AKT3 (83% of ctrl.); Follow up in vitro activity: IC50(AKT3) = 618 nM (HTFR assay, PMID: 31584233), IC50(AKT3) = 4.3 µM (NanoBRET assay)

Screened at 1 µM, 33P-ATP and filter-binding assay, closest target as % inhibition: BRK (99%), others >90%; In vitro potencies of closest 12 targets (33P-ATP and filter-binding assay (Reaction Biology)): IC50(ITK) = 56 nM, IC50(TEC) = 2.0 nM, IC50(JAK3) = 580 nM, IC50(EGFR) = 2.6 nM, IC50(HER2) = 530 nM, IC50(BRK) = 33 nM, IC50(FGR) = 155 nM, IC50(FRK/PTK5) = 379 nM, IC50(LCK) = 187 nM; Cellular selectivity: IC50(EGFR) = 606 nM (337-fold, p-EGFR HTRF assay), IC50(ITK) = 3477 nM (1932-fold, p-PLCg1 assay), IC50(TEC) = 204.7 nM (114-fold, p-TEC MSD assay), other targets not tested;

Screened at 1 µM, 33P-ATP and filter-binding assay, closest target as % inhibition: BRK (99%), others >90%; In vitro potencies of closest 12 targets (33P-ATP and filter-binding assay (Reaction Biology)): IC50(ITK) = 56 nM, IC50(TEC) = 2.0 nM, IC50(JAK3) = 580 nM, IC50(EGFR) = 2.6 nM, IC50(HER2) = 530 nM, IC50(BRK) = 33 nM, IC50(FGR) = 155 nM, IC50(FRK/PTK5) = 379 nM, IC50(LCK) = 187 nM; Cellular selectivity: IC50(EGFR) = 606 nM (337-fold, p-EGFR HTRF assay), IC50(ITK) = 3477 nM (1932-fold, p-PLCg1 assay), IC50(TEC) = 204.7 nM (114-fold, p-TEC MSD assay), other targets not tested;

Screened at 1 µM, 33P-ATP and filter-binding assay, closest target as % inhibition: BRK (99%), others >90%; In vitro potencies of closest 12 targets (33P-ATP and filter-binding assay (Reaction Biology)): IC50(ITK) = 56 nM, IC50(TEC) = 2.0 nM, IC50(JAK3) = 580 nM, IC50(EGFR) = 2.6 nM, IC50(HER2) = 530 nM, IC50(BRK) = 33 nM, IC50(FGR) = 155 nM, IC50(FRK/PTK5) = 379 nM, IC50(LCK) = 187 nM; Cellular selectivity: IC50(EGFR) = 606 nM (337-fold, p-EGFR HTRF assay), IC50(ITK) = 3477 nM (1932-fold, p-PLCg1 assay), IC50(TEC) = 204.7 nM (114-fold, p-TEC MSD assay), other targets not tested;

Screened at 1 µM, 33P-ATP and filter-binding assay, closest target as % inhibition: BRK (99%), others >90%; In vitro potencies of closest 12 targets (33P-ATP and filter-binding assay (Reaction Biology)): IC50(ITK) = 56 nM, IC50(TEC) = 2.0 nM, IC50(JAK3) = 580 nM, IC50(EGFR) = 2.6 nM, IC50(HER2) = 530 nM, IC50(BRK) = 33 nM, IC50(FGR) = 155 nM, IC50(FRK/PTK5) = 379 nM, IC50(LCK) = 187 nM; Cellular selectivity: IC50(EGFR) = 606 nM (337-fold, p-EGFR HTRF assay), IC50(ITK) = 3477 nM (1932-fold, p-PLCg1 assay), IC50(TEC) = 204.7 nM (114-fold, p-TEC MSD assay), other targets not tested;

Screened at 1 µM, 33P-ATP and filter-binding assay, closest target as % inhibition: BRK (99%), others >90%; In vitro potencies of closest 12 targets (33P-ATP and filter-binding assay (Reaction Biology)): IC50(ITK) = 56 nM, IC50(TEC) = 2.0 nM, IC50(JAK3) = 580 nM, IC50(EGFR) = 2.6 nM, IC50(HER2) = 530 nM, IC50(BRK) = 33 nM, IC50(FGR) = 155 nM, IC50(FRK/PTK5) = 379 nM, IC50(LCK) = 187 nM; Cellular selectivity: IC50(EGFR) = 606 nM (337-fold, p-EGFR HTRF assay), IC50(ITK) = 3477 nM (1932-fold, p-PLCg1 assay), IC50(TEC) = 204.7 nM (114-fold, p-TEC MSD assay), other targets not tested;

Tm panel screened at 20 µM, closest targets (dTm >5 K): dTm (CAMKK2) = 7.2 K, dTm(CLK1) = 6.4 K, dTm(EPHA2) = 6.2 K, dTm(NEK2) = 5.1 K, dTm(SRPK1) = 5.1 K, dTm(PHKG2) = 5.5 K, dTm(STK10) = 5.8 K, dTm(STK6) = 10.1 K, dTm(STK4) = 5.2 K, dTm(ULK3) = 5.8 K; Screened against 19 kinases (Radiometric inhibition assays): no target within 30-fold (PMID: 15323564)

Screened at 10 µM, closest target as % of contr.: PIK3CB (6.7%)

Screened at 10 µM, closest target as % of contr.: PIK3CB (6.7%)

Screened at 30 µM, highly specific

Screened at 30 µM, highly specific

Screened at 30 µM, highly specific

Screened at 30 µM, highly specific

In-vitro potencies of closest targets in the screen: Kd(MTOR) = 12 nM, Kd(HIPK3) = 310 nM, Kd(PIP5K2C) = 620 nM, Kd(RIOK2), Kd(DAPK3) = 840 nM, Kd(YSK4) = 930 nM, full screening data are available as supporting information;
Screened against 69 kinases at 1 µM, closest targets as % of control: SmMLCK (62%), HIPK2 (67%), full screening data available in paper, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2267365/;

In-vitro potencies of closest targets in the screen: Kd(MTOR) = 12 nM, Kd(HIPK3) = 310 nM, Kd(PIP5K2C) = 620 nM, Kd(RIOK2), Kd(DAPK3) = 840 nM, Kd(YSK4) = 930 nM, full screening data are available as supporting information;
Screened against 69 kinases at 1 µM, closest targets as % of control: SmMLCK (62%), HIPK2 (67%), full screening data available in paper, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2267365/;

In-vitro potencies of closest targets in the screen: Kd(MTOR) = 12 nM, Kd(HIPK3) = 310 nM, Kd(PIP5K2C) = 620 nM, Kd(RIOK2), Kd(DAPK3) = 840 nM, Kd(YSK4) = 930 nM, full screening data are available as supporting information;
Screened against 69 kinases at 1 µM, closest targets as % of control: SmMLCK (62%), HIPK2 (67%), full screening data available in paper, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2267365/;

In-vitro potencies of closest targets in the screen: Kd(MTOR) = 12 nM, Kd(HIPK3) = 310 nM, Kd(PIP5K2C) = 620 nM, Kd(RIOK2), Kd(DAPK3) = 840 nM, Kd(YSK4) = 930 nM, full screening data are available as supporting information;
Screened against 69 kinases at 1 µM, closest targets as % of control: SmMLCK (62%), HIPK2 (67%), full screening data available in paper, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2267365/;

In-vitro potencies of closest targets in the screen: Kd(MTOR) = 12 nM, Kd(HIPK3) = 310 nM, Kd(PIP5K2C) = 620 nM, Kd(RIOK2), Kd(DAPK3) = 840 nM, Kd(YSK4) = 930 nM, full screening data are available as supporting information;
Screened against 69 kinases at 1 µM, closest targets as % of control: SmMLCK (62%), HIPK2 (67%), full screening data available in paper, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2267365/;

In-vitro potencies of closest targets in the screen: Kd(MTOR) = 12 nM, Kd(HIPK3) = 310 nM, Kd(PIP5K2C) = 620 nM, Kd(RIOK2), Kd(DAPK3) = 840 nM, Kd(YSK4) = 930 nM, full screening data are available as supporting information;
Screened against 69 kinases at 1 µM, closest targets as % of control: SmMLCK (62%), HIPK2 (67%), full screening data available in paper, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2267365/;

Screened at 1 µM or 10 µM (iknase panel literature or Upstate/Millipore); Closest targets: Ki(VEGFR2) = 8 nM, IC50(YES) = 14 nM, IC50(FMS) = 10 nM, IC50(AURKA) = 23nM, IC50(FGFR3) = 23 nM, IC50(FLT3) = 25 nM, IC50(RET) = 39 nM;

Screened at 1 µM or 10 µM (Kinase panel literature or Upstate/Millipore); Closest targets: Ki(VEGFR2) = 8 nM, IC50(YES) = 14 nM, IC50(FMS) = 10 nM, IC50(AURKA) = 23nM, IC50(FGFR3) = 23 nM, IC50(FLT3) = 25 nM, IC50(RET) = 39 nM;

Screened at 10 µM, none target within 10-fold, closest target as % of contr.: PIK3CA (I800L, 33%)

Screened at 10 µM, none target within 10-fold, closest target as % of contr.: PIK3CA (I800L, 33%)

Kinases screened in Kinobeads assay,closest target: Kd(CAMKK2) = 195 nM; Kd (BRD4) = 79 nM.

Kinases screened in Kinobeads assay,closest target: Kd(CAMKK2) = 195 nM; Kd (BRD4) = 79 nM.

Kinases screened in Kinobeads assay,closest target: Kd(CAMKK2) = 195 nM; Kd (BRD4) = 79 nM.

In vitro activity of closest targets:IC50(FLT1/4) = 42/74 nM, IC50(TIE2) = 59 nM, IC50(SIK) = 70 nM, IC50(FGFR1) = 78 nM

In vitro activity of closest targets:IC50(FLT1/4) = 42/74 nM, IC50(TIE2) = 59 nM, IC50(SIK) = 70 nM, IC50(FGFR1) = 78 nM

Screened at 1 µM, closest targets as % of contr.: CDK9 (10%), FLT3(D835Y) (9%), PLK1 (3%); Screened additionally against 58 kinases (radiometric kinase assay), closesttargets: IC50(FLT3) = 510 nM, IC50(MELK) = 744 nM, IC50(CK2) = 826 nM, other targets IC50 >10 µM (PMID: 21470862)

Screened at 1 µM, closest targets: IC50(PRKD2) = 139 nM, IC50(PRKD3) = 219 nM, IC50(RET) = 161 nM, IC50(FLT3) = 714 nM, IC50(LRRK2) =16 nM, IC50(PRKD1) = 35 nM, IC50(CLK1/2) = 512/ 112 nM, IC50(FGFR2) = 320 nM, IC50(PDGFRA) = 956 nM; Screened against panel of 68 receptors, ion channels and protein targets, at 10 µM, closest targets: IC50(A1A) = 914 nM, IC50(A1B) = 52 nM, IC50(A1D) = NA, IC50(A2A) = 1420 nM, IC50(AB2) = 1820 nM, IC50(imidazoline I2) = 97 nM (PMID: 22128344)

In vitro inhibition (biochemical potency): >100 fold selective for MEK, other targets >10µM

Screened at 1 µM, closest targets as % of cont.: PIK3C2B (80.4%), PIK3CA (98.6%), PIK3CD (97.9%), PIK3CG (90.6%), PIK3C3 (69.9%); IC50 follow-up of closest targets: IC50(PIK3C2B) = 292 nM, IC50(PIK3C3) = 374 nM, >1000-fold selective

Screened at 1 µM, closest targets as % of cont.: PIK3C2B (80.4%), PIK3CA (98.6%), PIK3CD (97.9%), PIK3CG (90.6%), PIK3C3 (69.9%); IC50 follow-up of closest targets: IC50(PIK3C2B) = 292 nM, IC50(PIK3C3) = 374 nM, >1000-fold selective

Screened at 1 µM, closest targets as % of cont.: PIK3C2B (80.4%), PIK3CA (98.6%), PIK3CD (97.9%), PIK3CG (90.6%), PIK3C3 (69.9%); IC50 follow-up of closest targets: IC50(PIK3C2B) = 292 nM, IC50(PIK3C3) = 374 nM, >1000-fold selective

Screened at 1 µM, closest targets as % of cont.: PIK3C2B (80.4%), PIK3CA (98.6%), PIK3CD (97.9%), PIK3CG (90.6%), PIK3C3 (69.9%); IC50 follow-up of closest targets: IC50(PIK3C2B) = 292 nM, IC50(PIK3C3) = 374 nM, >1000-fold selective

Screened at 1 µM, closest target with PoC <10%: ABL2 (5.8%)

Screened at 1 µM, closest target with PoC <10%: ABL2 (5.8%)

Screened at 10 µM, S(10) = 0.007, closest targets as % of contr.: DCAMK2 (3.6%), PLK4 (5.1%); Cellular selectivity profiling at 10 µM using KiNativ method, only ERK5 inhibited with90 % higher target occupancy;

Screened at 10 µM, > 50-fold selective

Screened at 1 µM, closest targets: Ki(LTK) = 2.7 nM, Ki(FER) = 3.3 nM, Ki(FES) = 6 nM, Ki(PTK2B) = 14 nM, Ki(TNK2) = 17 nM, Ki(PTK2) = 17 nM, Ki(NTRK1) = 24 nM, Ki(NTKR2) = 23 nM, Ki(NTRK3) = 46 nM, Ki(FRK) = 53 nM, Ki(EGFR(L858R/T790M)) = 56 nM, Ki(EGFR(T790M) = 319 nM, Ki(JAK2) = 529 nM, others >75% inhibition at 1 µM

Screened at 1 µM, closest off-targets: Ki(LTK) = 2.7 nM, Ki(FER) = 3.3 nM, Ki(FES) = 6 nM, Ki(PTK2B) = 14 nM, Ki(TNK2) = 17 nM, Ki(PTK2) = 17 nM, Ki(NTRK1) = 24 nM, Ki(NTKR2) = 23 nM, Ki(NTRK3) = 46 nM, Ki(FRK) = 53 nM, Ki(EGFR(L858R/T790M)) = 56 nM, Ki(EGFR(T790M) = 319 nM, Ki(JAK2) = 529 nM, others >75% inhibition at 1 µM

Screened at 10 µM, closest targets with < 10% of contr.: GAK, JAK1, STK16, TTK, PIK3C2G, MAP2K4; Screened against 240 kinases (Milipore panel): >10000-fold selective

Screened at 10 µM, closest targets with < 10% of contr.: GAK, JAK1, STK16, TTK, PIK3C2G, MAP2K4; Screened against 240 kinases (Milipore panel): >10000-fold selective

Screened at 10 µM, closest targets with < 10% of contr.: GAK, JAK1, STK16, TTK, PIK3C2G, MAP2K4; Screened against 240 kinases (Milipore panel): >10000-fold selective

Screened at 10 µM, closest targets with < 10% of contr.: GAK, JAK1, STK16, TTK, PIK3C2G, MAP2K4; Screened against 240 kinases (Milipore panel): >10000-fold selective

Screened at 1 µM, closest target as % of contr.: CSNK1E (39%)

Screened at 1 µM, closest targets: IC50(FLT3) = 390 nM, IC50(KIT) = 860 nM, IC50(AURKC) = 1000 nM, IC50(KDR) = 1100 nM (enzymatic assay with 100 µM ATP), other targets > 1 µM; Cellular selectivity: IC50(FLT3) > 10 µM (FLT3-ITD dependent proliferation of Ba/F3 cells); IC50(KIT) = 2.7 µM (BCR-KIT fusion dependent proliferation of Ba/F3 cells)

Screened at 10 µM, closest targets as % of contr.: GAK(4.1%), RIOK1/3 (4.1/4.2%), PDGFRB (5.3%), FLT3(D835H)(1.4%), FLT4(1.4%), KIT(D816V)(1.4%), PIP5K2B(6.6%), MAPK3K1(1.6%), PIP5K2B(6.6%), DAPK1(8.6%), FLT3(N841I) (1.7%), ROCK1 (4.7%), MST2(1.8%), SRPK1(8.9%), EPHB6(9.9%), LOK(0.0%), PLK2(0.2%), SLK(0.3%), MP2K5(0.5%), BIKE(1.0%), PIP5K1C (10%); Screened against 30 kinases, closest targets: IC50(PDGFR1b) = 160 nM, IC50(VEGFR2) = 360 nM, IC50(AURA) = 4800 nM, IC50(CDK2/cyclinA) = 7600 nM, others IC50 >10 µM (PMID: 17267659)

Screened at 10 µM, closest targets as % of contr.: GAK(4.1%), RIOK1/3 (4.1/4.2%), PDGFRB (5.3%), FLT3(D835H)(1.4%), FLT4(1.4%), KIT(D816V)(1.4%), PIP5K2B(6.6%), MAPK3K1(1.6%), PIP5K2B(6.6%), DAPK1(8.6%), FLT3(N841I) (1.7%), ROCK1 (4.7%), MST2(1.8%), SRPK1(8.9%), EPHB6(9.9%), LOK(0.0%), PLK2(0.2%), SLK(0.3%), MP2K5(0.5%), BIKE(1.0%), PIP5K1C (10%); Screened against 30 kinases, closest targets: IC50(PDGFR1b) = 160 nM, IC50(VEGFR2) = 360 nM, IC50(AURA) = 4800 nM, IC50(CDK2/cyclinA) = 7600 nM, others IC50 >10 µM (PMID: 17267659)

Screened at 10 μM, closest targets at % of contr.: DDR1 (1.1%), FLT4 (6.0%), CSF1R (6.6%), MST3 (7.0%), VEGFR1 (8.0%), YSK1 (9.4%);In-vitro potency of other targets: IC50(PDGFR, cytoplasmic domain) = 17.6 µM, IC50(c-Src) = 19.8 µM;

Screened at 10 μM, closest targets at % of contr.: DDR1 (1.1%), FLT4 (6.0%), CSF1R (6.6%), MST3 (7.0%), VEGFR1 (8.0%), YSK1 (9.4%); In-vitro potency of other targets: IC50(PDGFR, cytoplasmic domain) = 17.6 µM, IC50(c-Src) = 19.8 µM;

Screened at 10 μM, closest targets at % of contr.: DDR1 (1.1%), FLT4 (6.0%), CSF1R (6.6%), MST3 (7.0%), VEGFR1 (8.0%), YSK1 (9.4%); In-vitro potency of other targets: IC50(PDGFR, cytoplasmic domain) = 17.6 µM, IC50(c-Src) = 19.8 µM;

Screened at 1 µM, closest targets as % of contr.: ABL1-nonphosphorylated (14%), RIPK2 (30%), RPS6KA5RPS6KA5(Kin.Dom.2-C-terminal) (35%), CHEK2 (37%), PIK3CA (37%), STK38L (40%); Follow-up IC50s in cellular NanoBRET assays: all targets IC50 >25 µM (>125-fold selective);

Screened at 1 µM, closest targets as % of contr.: ABL1-nonphosphorylated (14%), RIPK2 (30%), RPS6KA5RPS6KA5(Kin.Dom.2-C-terminal) (35%), CHEK2 (37%), PIK3CA (37%), STK38L (40%); Follow-up IC50s in cellular NanoBRET assays: all targets IC50 >25 µM (>125-fold selective);

Screened at 1 µM, closest targets as % of contr.: ABL1-nonphosphorylated (14%), RIPK2 (30%), RPS6KA5RPS6KA5(Kin.Dom.2-C-terminal) (35%), CHEK2 (37%), PIK3CA (37%), STK38L (40%); Follow-up IC50s in cellular NanoBRET assays: all targets IC50 >25 µM (>125-fold selective);

Screened at 1 µM, closest targets as % of contr.: ABL1-nonphosphorylated (14%), RIPK2 (30%), RPS6KA5RPS6KA5(Kin.Dom.2-C-terminal) (35%), CHEK2 (37%), PIK3CA (37%), STK38L (40%); Follow-up IC50s in cellular NanoBRET assays: all targets IC50 >25 µM (>125-fold selective);

Screened at 100 nM, closest targets: Kd(STK10) = 5.9 nM, Ki(EPHB6) = 25 nM, Ki(ABL-1, non-phosphorylated) = 38 nM, Ki(LYN) = 40 nM; Cellular selectivity, of closest targets in HEK293T cells (NanoBRET assay): IC50(STK10) = 210 ± 97 nM (n= 2), IC50(EPHB6) = 3.9 ± 0.3 µM (n= 2), IC50(LYN) = 8.2 ± 0.86 µM (n= 2); Screened against 45 GPCR targets (PDSP screen) at 10 µM, closest targets: Ki(OPRK1) = 124.61 nM, Ki(GABA/PBR) = 217.26 nM, Ki(TMEM97) = 983.68 nM, Ki(ADRB3) = 7099.67 nM

Screened at 100 nM, closest targets: Kd(STK10) = 5.9 nM, Ki(EPHB6) = 25 nM, Ki(ABL-1, non-phosphorylated) = 38 nM, Ki(LYN) = 40 nM; Cellular selectivity, of closest targets in HEK293T cells (NanoBRET assay): IC50(STK10) = 210 ± 97 nM (n= 2), IC50(EPHB6) = 3.9 ± 0.3 µM (n= 2), IC50(LYN) = 8.2 ± 0.86 µM (n= 2); Screened against 45 GPCR targets (PDSP screen) at 10 µM, closest targets: Ki(OPRK1) = 124.61 nM, Ki(GABA/PBR) = 217.26 nM, Ki(TMEM97) = 983.68 nM, Ki(ADRB3) = 7099.67 nM

Screened at 100 nM, closest targets: Kd(STK10) = 5.9 nM, Ki(EPHB6) = 25 nM, Ki(ABL-1, non-phosphorylated) = 38 nM, Ki(LYN) = 40 nM; Cellular selectivity, of closest targets in HEK293T cells (NanoBRET assay): IC50(STK10) = 210 ± 97 nM (n= 2), IC50(EPHB6) = 3.9 ± 0.3 µM (n= 2), IC50(LYN) = 8.2 ± 0.86 µM (n= 2); Screened against 45 GPCR targets (PDSP screen) at 10 µM, closest targets: Ki(OPRK1) = 124.61 nM, Ki(GABA/PBR) = 217.26 nM, Ki(TMEM97) = 983.68 nM, Ki(ADRB3) = 7099.67 nM

Screened at 100 nM, closest targets: Kd(STK10) = 5.9 nM, Ki(EPHB6) = 25 nM, Ki(ABL-1, non-phosphorylated) = 38 nM, Ki(LYN) = 40 nM; Cellular selectivity, of closest targets in HEK293T cells (NanoBRET assay): IC50(STK10) = 210 ± 97 nM (n= 2), IC50(EPHB6) = 3.9 ± 0.3 µM (n= 2), IC50(LYN) = 8.2 ± 0.86 µM (n= 2); Screened against 45 GPCR targets (PDSP screen) at 10 µM, closest targets: Ki(OPRK1) = 124.61 nM, Ki(GABA/PBR) = 217.26 nM, Ki(TMEM97) = 983.68 nM, Ki(ADRB3) = 7099.67 nM

Screened at 1 µM, no targets within 10-fold, closest kinases IC50 >100-fold

Screened at 1 µM, >100-fold selective, closest targets: IC50(CLK4) = 225 nM, IC50(MAP3K14) = 244 nM, IC50(MAP3K5) = 428 nM, IC50(CLK2) = 605 nM, IC50(TTK) = 935 nM); PanLabs Profile showed 5 hits > 50% inhibition at 10 µM: IC50 (HTR2B) = 1.2 µM, IC50(SLC6A2) = 3.8 µM, IC50(CHRM2) = 6.4 µM, IC50(PPARG) = 6.5 µM, IC50(adenosine transporter) = 9.7 µM; Screened against 45 GPCR targets (PDSP screen) at 10 µM, closest target: Ki(TMEM97) = 4600.45 nM

Screened at 100 nM, closest targets as % of contr.: LATS2 (0.7%), PRKACA (28%), PRKACB (36%), LATS1 (42%), PRKG1 (49%); Screened in Upstate kinase panel against 114 kinases at 10 µM, >250 fold selective, closest targets: IC50(NTRK1) = 252 nM, IC50(FLT3) = 303 nM, IC50(PKA) = 734 nM; Screened against 45 GPCR targets (PDSP screen), closest targets: Ki(OPRK1) = 187.33 nM, Ki(SIGMAR1) = 6765.5 nM; Screened in Eurofins-Panlabs radioligand binding assay against 63 targets at 10 µM, closest targets: Ki(SLC6A3) = 0.039 µM, Ki(DAT2) = 0.027 µM;