Selectivity data panels

Access and download selectivity data for the following molecule classes

Enzyme

Target & molecule name	Molecule selectivity data	Negative control selectivity data
AUTOTAXIN (ATX) INHIBITOR | BI-2545	ATX_BI-2545_selectivityData.xlsx	BI-3017_selectivityData.xlsx
CATC SUBSTRATE | BI-1750	BI-1750_selectivityData.xlsx	not applicable
CATHEPSIN C (CTSC) INHIBITOR | BI-9740	BI-9740_selectivityData.xlsx	BI-1821_selectivityData.xlsx
CHYMASE INHIBITOR | BI-1942	BI-1942_selectivityData.xlsx	BI-1829_selectivityData.xlsx
DPAP1 INHIBITOR | BI-2051	BI-2051_selectivityData.xlsx	BI-2054_selectivityData.xlsx
FAS INHIBITOR | BI 99179	BI-99179_selectivityData.xlsx	BI 99990_selectivityData.xlsx
FLAP ANTAGONIST | BI 665915	BI-665915_selectivityData.xlsx	BI-0153_selectivityData.xlsx
HCV NS5B POLYMERASE INHIBITOR | BI 207127 (DELEOBUVIR)	BI 207127_selectivityData.xlsx	BI-7656_selectivityData.xlsx
HCV PROTEASE INHIBITOR | BI-1230	BI-1230_selectivityData.xlsx	BI-1675_selectivityData.xlsx
HCV PROTEASE INHIBITOR FALDAPREVIR | BI 201335	BI-201335_selectivityData.xlsx	BI-1675_selectivityData.xlsx
HCV PROTEASE INHIBITOR | BI-1388	BI-1388_selectivityData.xlsx	no negative control available
HCV POLYMERASE INHIBITOR | BI-0588	BI-0588_selectivityData.xlsx	BI-0900_selectivityData.xlsx
HIV NNRTI | BI-2540	BI-2540_selectivityData.xlsx	BI-2439_selectivityData.xlsx
HIV INTEGRASE INHIBITOR | BI 224436	BI 224436_selectivityData.xlsx	BI-0449_selectivityData.xlsx
MMP-13 ANTAGONIST | BI-4394	BI-4394_selectivityData.xlsx	BI-4395_selectivityData.xlsx
SEH INHIBITOR | BI-1935	BI-1935_selectivityData.xlsx	BI-2049_selectivityData.xlsx
STEP ACTIVATOR | BI-0314	BI-0314_selectivityData.xlsx	no negative control available
TELOMERASE INHIBITOR | BIBR1532	BIBR1532_selectivityData.xlsx	BIBR1654_selectivityData.xlsx
Cathepsin S inhibitor | BI-1124	BI-1124_selectivityData_1.xlsx	BI-1920_selectivityData.xlsx
Cathepsin S inhibitor | BI-1915	BI-1915_selectivityData2.xlsx	BI-1920_selectivityData_1.xlsx
PHGDH inhibitor | BI-4916	BI-4916_selectivityData.xlsx	BI-5583_selectivityData.xlsx
PHGDH Inhibitor | BI-4924	BI-4924_selectivityData.xlsx	BI-5583_selectivityData.xlsx
Neutrophil Elastase inhibitor | BI-5524	BI-5524_selectivityData.xlsx	BI-5525_selectivityData.xlsx
CMV polymerase inhibitor | BI-9553	BI-9553_selectivityData.xlsx	BI-0309_selectivityData.xlsx
HSD17B13 inhibitor | BI-3231	BI-3231_selectivityData.xlsx	BI-0955_selectivityData.xlsx
Orally bioavailable PHGDH inhibitor | BI-9593	BI-9593_selectivityData.xlsx	BI-9594_selectivityData.xlsx
Bacterial PROTAC | BI-8255	BI-8255_selectivityData_0.xlsx	BI-8256_selectivityData.xlsx
GCH1 inhibitor | AXSP0056BS	AXSP0056_selectivityData.xlsx	DX-0373_selectivityData.xlsx
Dual Vanin Inhibitor | BI-4122	BI-4122_selectivityData.xlsx	BI-9534_selectivityData.xlsx
PDE9 inhibitor | BI 409306	BI-409306_selectivityData.xlsx	negative control available

Epigenetic
target

Target & molecule name	Molecule selectivity data	Negative control selectivity data
BET PROTAC | MZ1	MZ_1_selectivityData.xlsx	cis_MZ_1_selectivityData.xlsx
BRD7/BRD9 INHIBITOR | BI-7273	BI-7273_selectivityData.xlsx	BI-6354_selectivityData.xlsx
BRD7/BRD9 PROTAC | VZ185	VZ185_selectivityData.xlsx	cis_VZ185_selectivityData.xlsx
BRD9 INHIBITOR | BI-9564	BI-9564_selectivityData.xlsx	BI-6354_selectivityData.xlsx
NSD3-PWWP1 ANTAGONIST | BI-9321	BI-9321_selectivityData.xlsx	BI-9466_selectivityData.xlsx
SMARCA2/4 PROTAC | ACBI1	ACBI1_selectivityData.xlsx	ACBI1_neg_ctrl_selectivityData.xlsx
MLKL inhibitor | BI-8925	BI-8925_selectivityData.xlsx	BI-8762_selectivityData.xlsx
BPTF inhibitor | BI-7190	BI-7190_selectivityData.xlsx	BI-4827_selectivityData.xlsx
SMARCA2 PROTAC | ACBI2	ACBI2_selectivityData.xlsx	cis-ACBI2_selectivityData.xlsx
Orally bioavailable BET inhibitor | BI 894999	BI894999_selectivityData.xlsx	Data in the process of being generated

GPCR

Target & molecule name	Molecule selectivity data	Negative control selectivity data
5-HT2C RECEPTOR AGONISTS | BI-4752 AND BI-3234	BI-4752_selectivityData.xlsx	BI-3234_selectivityData.xlsx
β2AR AGONIST | BI-167107	BI-167107_selectivityData.xlsx	no negative control available
CCR10 ANTAGONIST | BI-6901	BI-6901_selectivityData.xlsx	BI-6902_selectivityData.xlsx
CCR1 ANTAGONIST | BI 639667	BI-639667_selectivityData.xlsx	BI-9307_selectivityData.xlsx
LTB4 ANTAGONIST | BIIL 284	BIIL-284_selectivityData.xlsx	BIIS035_selectivityData.xlsx
LTB4 RECEPTOR ANTAGONIST | BIIL 315	BIIL-315_selectivityData.xlsx	BIIS035_selectivityData.xlsx
GPR40 agonist | BI-2081	BI-2081_selectivityData.xlsx	BI-0340_selectivityData.xlsx
NPY2R Antagonist | BIIE0246	BIIE0246_selectivityData.xlsx	BIIE0212_selectivityData.xlsx
GPR142 Agonist | BI-1046	BI-1046_selectivityData.xlsx	BI-4420_selectivityData.xlsx
Apafant | PAF Receptor Antagonist	WEB2086BS_selectivityData.xlsx	WEB2387BS_selectivityData.xlsx
Bepafant | PAF Receptor Antagonist	Bepafant_selectivityData.xlsx	WEB2387BS_selectivityData.xlsx
S-Bepafant | PAF Receptor Antagonist	WEB2388_selectivityData.xlsx	WEB2387BS_selectivityData.xlsx
NPY1R Antagonist | BIBO3304	BIBO3304_selectivityData.xlsx	BIBO3457_selectivityData.xlsx
B1 receptor antagonist | BI113823	BI113823_selectivityData.xlsx	BI-5832_selectivityData.xlsx
Beta-3 adrenergic receptor agonist | BI-2800	BI-2800_selectivityData.xlsx	BI-0962_selectivityData.xlsx
Secretin Receptor Agonist | BI-3434	BI-3434_selectivityData.xlsx	no negative control available
GPR88 agonist | BI-9508	BI-9508_selectivityData.xlsx	BI-0823_selectivityData.xlsx
OX1 receptor antagonist | BI-5121	BI-5121_selectivityData.xlsx	BI-6199_selectivityData.xlsx
mGluR2 Positive Allosteric Modulator | BI-4737	BI-4737_selectivityData.xlsx	BI-4576_selectivityData.xlsx
mGluR1 Positive Allosteric Modulators | BI02982816	BI-2816_selectivityData.xlsx	BI-4066_selectivityData.xlsx

ION channel

Target & molecule name	Molecule selectivity data	Negative control selectivity data
NAV1.2 CHANNEL BLOCKER | BIII 890CL (CROBENETINE)	BIII890CL_selectivityData.xlsx	BI-355CL_selectivityData.xlsx
NHE1 INHIBITOR | BI-9627	BI-9627_selectivityData.xlsx	BI-0054_selectivityData.xlsx
NMDA RECEPTOR ANTAGONIST | BIII 277CL	BIII-277CL_selectivityData.xlsx	BI-25CL_selectivityData.xlsx
ENaC Inhibitor | BI-8668	BI-8668_selectivityData.xlsx	BI-0337_selectivityData.xlsx
GABAA alpha5 | BI-1030	BI-1030_selectivityData.xlsx	no negative control available
Voltage-gated Na+ channel 1.1 activator | BI-7150	BI-7150_selectivityData.xlsx	BI-7283_selectivityData.xlsx
Slowpoke 1 (SLO-1) channel agonist | BI-3972	BI-3972_selectivityData.xlsx	BI-4083_selectivityData.xlsx
TRPC4/5 inhibitor | HC-070	ongoing	no negative control available

Kinase

Target & molecule name	Molecule selectivity data	Negative control selectivity data
ALK5 INHIBITOR | BI-4659	BI-4659_selectivityData.xlsx	BI-4101_selectivityData.xlsx
AURORA B INHIBITOR | BI 831266	BI-831266_selectivityData.xlsx	BI-1282_selectivityData.xlsx
CDK8 INHIBITOR | BI-1347	BI-1347_selectivityData.xlsx	BI-1374_selectivityData.xlsx
GSK-3 INHIBITOR | BI-5521	BI-5521_selectivityData.xlsx	BI-4481_selectivityData.xlsx
IKKβ INHIBITOR | BI 605906	BI-605906_selectivityData.xlsx	BI-5026_selectivityData.xlsx
PLK1 INHIBITOR | BI-2536	BI-2536_selectivityData.xlsx	no negative control available
PTK2 PROTAC | BI-0319	BI-0319_selectivityData.xlsx	BI-4206_selectivityData.xlsx
PTK2 PROTAC | BI-3663	BI-3663_selectivityData.xlsx	BI-4206_selectivityData.xlsx
SYK INHIBITOR | BI 1002494	BI-1002494_selectivityData.xlsx	BI-2492_selectivityData.xlsx
AMPK Activator | BI-9774	BI-9774_selectivityData.xlsx	no negative control available
P38 MAPK Inhibitor | BIRB 796	BIRB-796_selectivityData.xlsx	no negative control available
RSK Inhibitor | BIX 02565	BIX-02565_selectivityData.xlsx	no negative control available
EGFR inhibitor | BI-8128	BI-8128_selectivityData.xlsx	no negative control available
KHK inhibitor | BI-9787	BI-9787_selectivityData.xlsx	BI-2817_selectivityData.xlsx
EGFR inhibitor | BI-4732	BI-4732_selectivityData.xlsx	BI-8218_selectivityData.xlsx
IRAK4 inhibitor | BI1543673	BI1543673_selectivityData.xlsx	BI-4326_selectivityData.xlsx
PI3K gamma inhibitor | BI-9222	BI-9222_selectivityData.xlsx	BI-9183_selectivityData.xlsx

Membrane transporter

Target & molecule name	Molecule selectivity data	Negative control selectivity data
LOX-1 INHIBITOR | BI-0115	BI-0115_selectivityData.xlsx	BI-1580_selectivityData.xlsx
SLC13A5 INHIBITOR | BI01383298	BI01383298_selectivityData.xlsx	BI-2674_selectivityData.xlsx
CETP inhibitor | BI-5756	BI-5756_selectivityData.xlsx	BI-9313_selectivityData.xlsx
MRP4 inhibitor | BI-4926	BI-4926_selectivityData.xlsx	BI-5106_selectivityData.xlsx

Nuclear receptor

Target & molecule name	Molecule selectivity data	Negative control selectivity data
GLUCOCORTICOID RECEPTOR (GR) AGONIST | BI 653048	BI-653048_selectivityData.xlsx	BI-3047_selectivityData.xlsx

PPI

Target & molecule name	Molecule selectivity data	Negative control selectivity data
BCL6 DEGRADER | BI-3802	BCL6-degr_BI-3802_selectivityData.xlsx	BI-5273_selectivityData.xlsx
BCL6 INHIBITOR | BI-3812	BI-3812_selectivityData.xlsx	BI-5273_selectivityData.xlsx
KRAS switch I/II pocket inhibitor | BI-2852	BI-2852_selectivityData.xlsx	BI-2853_selectivityData.xlsx
LFA-1 ANTAGONIST | BI-1950	BI-1950_selectivityData.xlsx	BI-9446_selectivityData.xlsx
Capsid Assembly Inhibitor | BI-3257	BI-3257_selectivityData.xlsx	BI-3545_selectivityData.xlsx
SOS1::KRAS inhibitor | BI-3406	BI-3406_selectivityData.xlsx	BI-0178_selectivityData.xlsx
SOS1 Activator | VUBI1	VUBI1_selectivityData.xlsx	BI-9930_selectivityData.xlsx
KRAS G12C inhibitor | BI-0474	BI-0474_selectivityData.xlsx	bi-0473_selectivitydata.xlsx
MDM2–p53 antagonist | BI-0282	BI-0282_selectivityData.xlsx	bi-0283_selectivitydata.xlsx

RNA Target

Target & molecule name	Molecule selectivity data	Negative control selectivity data
TPP Riboswitch activator | BI-5232	BI-5232_selectivityData.xlsx	ongoing

References

1. Eurofins Discovery Press Release, September 21, 2020
2. Arrowsmith C.H., Audia J.E., Austin C., Baell J., Bennett J., Blagg J., Bountra C., Brennan P.E., Brown P.J., Bunnage M.E., Buser-Doepner C., Campbell R.M., Carter A.J., Cohen P., Copeland R.A., Cravatt B., Dahlin J.L., Dhanak D., Edwards A.M., Frederiksen M., Frye S.V., Gray N., Grimshaw C.E., Hepworth D., Howe T., Huber K.V.M., Jin J., Knapp S., Kotz J.D., Kruger R.G., Lowe D., Mader M.M., Marsden B., Mueller-Fahrnow A., Müller S., O'Hagan R.C., Overington J.P., Owen D.R., Rosenberg S.H., Roth B., Roth B., Ross R., Schapira M., Schreiber S.L., Shoichet B., Sundström M., Superti-Furga G., Taunton J., Toledo-Sherman L., Walpole C., Walters M.A., Willson T.M., Workman P., Young R.N., Zuercher W.J. The promise and peril of chemical probes Nature Chemical Biology 2015, 11, 536-541. DOI, PubMed.
3. Kroeze W. K., Sassano M. F., Huang X. P., Lansu K., McCorvy J. D., Giguère P. M., Sciaky N., Roth B. L. PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome Nat Struct Mol Biol. 2015, 22(5):362-9. DOI, PubMed.