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"Molecules for Collaboration" (M4C) offers the opportunity to initiate joint research projects. We invite scientists and researchers who are interested in our well-characterized, but unpublished molecules to submit their research proposals addressing a novel scientific idea. If your proposal is chosen, the project will be pursued as part of a bi-lateral partnership with us.


β2AR
BI-167107

β2 adrenergic receptor (β2AR ) agonists have been used as bronchodilating agents for the last decades for the treatment of pulmonary diseases like asthma. BI-167107 was synthesized during a campaign to develop third generation of β2-agonists suitable for a once a day regimen. Due to its high potency and slow dissociation from the target it was subsequently used to support crystallization of active state β2AR and β2AR-G-protein complexes.

SYK
BI 1002494

BI 1002494 is due to its high potency, good physicochemical properties, suitable selectivity profile and low toxicity an excellent tool to explore SYK functions in vitro and in vivo.

sEH
BI-1935

BI-1935 is a potent and selective small molecule inhibitor of Soluble epoxide hydrolase (sEH). In a biochemical binding assay h-sEH it shows an IC50 of 7 nM and is also highly active in a cellular Hep G2-DHET assay format (IC50 < 1 nM).

PLK1
BI-2536

BI-2536 was the first potent and selective PLK1 inhibitor which entered clinical trials. It is a suitable in vitro and in vivo tool to study PLK function.

NHE1
BI-9627

BI-9627 is a highly potent NHE1 inhibitor with low DDI potential, excellent pharmacokinetics, and good selectivity against NHE2 and NHE3.

MMP-13
BI-4394

BI-4394 is a potent and highly selective inhibitor of MMP-13 that can be used as tool compound to test biological hypotheses in vitro.

LFA-1
BI-1950

BI-1950 potently inhibits the binding of LFA-1 to ICAM-1 with a KD value of 9 nM and the production of IL-2 in human PBMC and whole blood with an IC50 value of 3 nM and 120 nM, respectively.

HCV NS3
BI-1388

BI-1388 is a nanomolar to picomolar inhibitor of HCV NS3 protease activity and of viral replication for various HCV genotypes and for resistant mutants D168V and R155K.

HCV NS3
BI-1230

BI-1230 is a single digit nanomolar inhibitor of HCV NS3 protease activity and of viral replication. BI-1230 was shown to be highly selective against other serine/cysteine proteases and to be suitable for in vivo studies.

HCV NS5B
BI 207127

BI 207127 (deleobuvir) is a highly potent inhibitor of the enzymatic function of NS5B, the RNA polymerase of HCV, and of viral replication  (~20 nM).

GR
BI 653048

BI 653048 is a “dissociated” GR agonist (displaying different transcriptional regulatory profiles between gene transrepression and transactivation) with selectivity for other nuclear receptors (MR, PR) and good drug-like properties.

FLAP
BI 665915

BI 665915 demonstrates nanomolar FLAP binding potency and is a molecule suitable for testing biological hypotheses in vitro and also in vivo.

FAS
BI 99179

Our FAS in vivo tool compound BI 99179 is characterised by high potency, good selectivity and significant peripheral and central exposure upon oral administration in rats.

CDK8
BI-1347

BI-1347 is a selective nanomolar CDK8 inhibitor, suitable for testing biological hypotheses in vitro and also in vivo.

CCR10
BI-6901

Our compound is the first small molecule inhibitor of the Chemokine receptor CCR10.1-3 It is a potent and selective compound and suitable for in vivo validation.

CCR1
BI 639667

BI 639667 is a potent, selective human CCR1 antagonist with optimized drug-like properties.

BRD9
BI-9564

BI-9564 binds with high affinity to BRD9 KD(BRD9, ITC) = 14 nM and with lower affinity to closely related BRD7 KD(BRD7, ITC) = 239 nM. CECR2 was the only other identified off-target (KD(CECR2, ITC) = 258 nM), but with no effect in cells at 1 µM (FRAP assay). BI-9464 is completely negative on BET family members in the AlphaScreen (>100 µM).

BRD7/BRD9
BI-7273

BI-7273 is a potent dual BRD7/BRD9 inhibitor with 30 fold better potency in the BRD7 AlphaScreen assay compared to our more selective BRD9 inhibitor BI-9564.

BCL6
BI-3812

BI-3812 is a single digit nanomolar BCL6::Co-repressor inhibitor which also inhibits the BCL6::Co-repressor complex formation in cells (IC50 = 40 nM). BI-3812 is a classical PPI inhibitor probe compound for testing hypotheses around BCL6 biology in vitro.

BCL6
BI-3802

BI-3802 is a single digit nanomolar BCL6::Co-repressor inhibitor which induces efficacious BCL6 protein degradation in several Diffuse large B-cell lymphoma (DLBCL) cell lines (e.g., DC50 = 20 nM in SU-DHL-4 cells).

ATX
BI-2545

BI-2545 inhibits human ATX with an IC50 of 2.2 nM. In human whole blood BI-2545 inhibits Autotaxin with an IC50 of 29 nM and in rat whole blood with an IC50 of 96 nM.

Aurora B
BI 831266

BI 831266 is a potent and selective Aurora B inhibitor that inhibits cell proliferation and could be used as tool compound testing biological hypotheses.