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T3-CLK

Compound concentration: 10 µM

Receptor	HGNC target name	Inhibition [%] (Primary experimental value)	Ki [nM] (Secondary experimental value)	pKi
Beta1	ADRB1	-7.22
Beta3	ADRB3	-11.51
H1	HRH1	54.89	2154.79 average (n=2)	5.67
H2	HRH2	19.41
5-HT1A	HTR1A	-11.70
5-HT1B	HTR1B	7.83
5-HT1D	HTR1D	5.95
Sigma 1	SIGMAR1	16.86
Sigma 2	TMEM97	13.44
5-HT1E	HTR1E	-1.52
5-HT2A	HTR2A	-2.63
5-HT2B	HTR2B	-7.63
5-HT2C	HTR2C	12.44
5-HT3	HTR3A	1.81
5-HT5A	HTR5A	4.00
5-HT6	HTR6	-15.74
5-HT7A	HTR7	-5.21
GABAA/BZP		7.47
D1	DRD1	4.41
D2	DRD2	10.85
D3	DRD3	12.75
D4	DRD4	9.12
DAT	SLC6A3	8.33
DOR	OPRD1	4.05
KOR	OPRK1	-6.32
MOR	OPRM1	5.33
Alpha1A	ADRA1A	-5.18
Alpha1B	ADRA1B	4.68
Alpha1D	ADRA1D	-12.43
Alpha2A	ADRA2A	2.61
Alpha2B	ADRA2B	19.27
Alpha2C	ADRA2C	17.17
D5	DRD5	-7.30
M1	CHRM1	-10.83
M3	CHRM3	21.12
M4	CHRM4	25.17
M5	CHRM5	9.31
NET	SLC6A2	5.30
GABA/PBR		-18.71
H3	HRH3	16.64
M2	CHRM2	3.82
SERT	SLC6A4	-3.55
Beta2	ADRB2	16.61
H4	HRH4	0.74
GABAA		-5.11

T3-CLK-N

Compound concentration: 10 µM

Receptor	HGNC target name	Inhibition [%] (Primary experimental value)	Ki [nM] (Secondary experimental value)	pKi
Sigma 2	TMEM97	97.92	411.90 average (n=2)	6.39
5-HT1E	HTR1E	60.45	3555.25 average (n=2)	5.46
5-HT2C	HTR2C	82.98	1066.46 average (n=2)	5.98
5-HT3	HTR3A	6.47
5-HT5A	HTR5A	83.24	2494.89 average (n=2)	5.65
5-HT6	HTR6	30.77
5-HT7A	HTR7	45.25
Alpha2A	ADRA2A	83.67	2658.89	5.58
Alpha2B	ADRA2B	77.56	1646.19 average (n=2)	5.79
Alpha2C	ADRA2C	88.54	> 10000.00 average (n=3)	< 5.00
Beta3	ADRB3	78.09	> 10000.00 average (n=2)	< 5.00
GABAA/BZP		13.48
D2	DRD2	57.48	2752.36 average (n=2)	5.63
D4	DRD4	34.78
DAT	SLC6A3	-0.51
DOR	OPRD1	46.16
KOR	OPRK1	54.39	990.27 average (n=2)	6.01
MOR	OPRM1	55.67	4021.59 average (n=2)	5.40
SERT	SLC6A4	26.33
Sigma 1	SIGMAR1	90.03	798.34 average (n=2)	6.13
5-HT2A	HTR2A	92.34	1526.37 average (n=3)	5.88
5-HT2B	HTR2B	44.06
Alpha1A	ADRA1A	66.42	1394.62 average (n=2)	5.87
Alpha1D	ADRA1D	57.00	1453.09 average (n=2)	5.84
Beta1	ADRB1	27.98
Beta2	ADRB2	17.20
D1	DRD1	58.21	1496.83 average (n=2)	5.89
D3	DRD3	78.87	2249.15 average (n=2)	5.72
D5	DRD5	29.67
GABAA		4.08
H1	HRH1	83.01	1901.20 average (n=3)	5.88
H2	HRH2	86.75	1725.74 average (n=2)	5.79
H3	HRH3	43.77
H4	HRH4	31.89
M1	CHRM1	68.31	2092.27 average (n=2)	5.71
M3	CHRM3	40.35
M4	CHRM4	0.99
M5	CHRM5	30.78
NET	SLC6A2	40.84
GABA/PBR		-6.10
5-HT1A	HTR1A	51.29	2557.41 average (n=2)	5.60
M2	CHRM2	6.55
5-HT1B	HTR1B	66.90	2168.63 average (n=2)	5.70
5-HT1D	HTR1D	50.55	3073.30 average (n=2)	5.55
Alpha1B	ADRA1B	50.45	5525.80 average (n=2)	5.27

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T3-CLK

Results are expressed as percent inhibition of control specific binding (mean values; n=2). Shown are supplementary data from PMID: 28232751 .

Conclusion: No additional kinases beyond the CMGC group of kinases were inhibited in this panel.

Target protein	HGNC name	Species	% inhibition at 1 µM	% inhibition at 1.11 µM	% inhibition at 0.1 µM	% inhibition at 0.123 µM
CLK1	CLK1			99.13		91.21
CLK2	CLK2			100.48		92.10
CLK3	CLK3			88.72		38.33
DYRK1A	DYRK1A			97.46		74.17
DYRK1B	DYRK1B			94.08		62.70
DYRK3	DYRK3			3.70		-1.82
DYRK4	DYRK4			-2.87		-8.38
SRPK1	SRPK1			-2.58		-3.09
SRPK2	SRPK2			5.16		1.82
ABL1	ABL1		55.7		10.14
AKT1 (PKB alpha)	AKT1		-11.8		-8.24
AMPK A1/B1/G1	PRKAA1 PRKAB1 PRKAG1		0.5		-2.00
AURKA (Aurora A)	AURKA		8.6		4.51
AURKB (Aurora B)	AURKB		16.1		6.77
AXL	AXL		-13.7		-10.19
BRAF	BRAF		17.2		8.71
CDK1/cyclin B	CDK1		7.1		7.95
CDK2/cyclin A	CDK2 CCNA2		3.3		0.33
CDK5/p25	CDK5 CDK5R1		0.8		1.84
CDK5/p35	CDK5 CDK5R1		-1.1		1.85
CHEK1 (CHK1)	CHEK1		18.4		9.74
CHEK2 (CHK2)	CHEK2		24.2		21.89
CSNK1A1 (CK1 alpha 1)	CSNK1A1		-2.7		-3.75
CSNK1D (CK1 delta)	CSNK1D		4.3		-2.92
EGFR (ErbB1)	EGFR		-16.6		-19.66
EPHA1	EPHA1		-0.6		-1.64
EPHA2	EPHA2		-6.3		-4.09
EPHA5	EPHA5		-5.0		-5.80
EPHB1	EPHB1		4.1		4.83
ERBB2 (HER2)	ERBB2		-28.0		-21.31
FGFR1	FGFR1		9.2		4.26
FLT1 (VEGFR1)	FLT1		-11.2		-15.17
FRAP1 (mTOR)	MTOR		-8.5		-5.58
GSK3B (GSK3 beta)	GSK3B		-3.1		-3.21
HIPK1 (Myak)	HIPK1		2.7		-0.71
HIPK2	HIPK2		-1.8		-3.60
IKBKB (IKK beta)	IKBKB		-4.7		-6.11
IRAK4	IRAK4		42.4		25.34
JAK1	JAK1		-27.0		10.93
JAK2	JAK2		-6.3		-7.35
KIT	KIT		37.5		10.97
MAP2K1 (MEK1)	MAP2K1		10.9		12.37
MAP2K2 (MEK2)	MAP2K2		13.8		16.95
MAPK1 (ERK2)	MAPK1		4.0		2.74
MAPK11 (p38 beta)	MAPK11		0.9		0.67
MAPK14 (p38 alpha)	MAPK14		6.4		4.88
MAPK3 (ERK1)	MAPK3		6.1		5.63
MAPK8 (JNK1)	MAPK8		2.6		5.45
MAPK9 (JNK2)	MAPK9		-1.5		3.18
MAPKAPK2	MAPKAPK2		2.1		3.68
MET (cMet)	MET		-7.4		-16.16
NEK1	NEK1		25.1		3.86
NEK2	NEK2		24.3		11.86
PDK1 Direct	PDK1		1.9		-0.83
PIM1	PIM1		11.3		15.55
PLK1	PLK1		2.5		7.85
PRKACA (PKA)	PRKACA		3.6		-1.57
PRKCA (PKC alpha)	PRKCA		3.7		4.38
PRKCQ (PKC theta)	PRKCQ		4.2		5.46
PTK2 (FAK)	PTK2		-7.4		-9.12
RET	RET		-2.4		-1.05
ROCK1	ROCK1		9.4		5.17
ROS1	ROS1		-0.4		-3.68
RPS6KB1 (p70S6K)	RPS6KB1		0.7		2.21
SRC	SRC		46.7		13.15
TEK (Tie2)	TEK		-0.3		0.11
CAMK1 (CaMK1)	CAMK1		5.3		7.14
CDK7/cyclin H/MNAT1	CDK7		-3.4		0.55
CDK9/cyclin T1	CDK9		-17.0		-13.96
DAPK1	DAPK1		-6.4		-4.42
PIK3CA/PIK3R1 (p110 alpha/p85 alpha)	PIK3CA PIK3R1		3.6		3.58