DarkKinome

The DarkKinome refers to a subset of protein kinases that are less studied compared to their more prominent counterparts. These kinases, including BRSK2, CDK10, CDK12, CDK13, DYRK1B, PIP4K2C, PKMYT1, STK17B, TLK2, and WEE2, are characterized by limited structural and functional knowledge, which poses challenges for drug discovery. Despite this, they are considered druggable targets due to their roles in various signaling pathways and potential implications in diseases such as cancer and neurodegeneration.

Target Kinases:

1. BRSK2: Involved in regulating neuronal function.

2. CDK10: Plays a role in cell cycle regulation and transcription.

3. CDK12: Important for RNA polymerase II transcriptional regulation.

4. CDK13: Functions similarly to CDK12 in transcriptional control.

5. DYRK1B: Associated with neurodevelopmental disorders and cancer.

6. PIP4K2C: Involved in phosphoinositide metabolism.

7. PKMYT1: Regulates cell cycle progression.

8. STK17B: Implicated in stress response pathways.

9. TLK2: Associated with DNA damage response.

10. WEE2: A critical regulator of the cell cycle.

To advance the understanding and therapeutic targeting of these dark kinases, we have created a specialized chemical library containing potential active 8436 molecules aimed at these targets. The development of this library utilizes machine learning algorithms combined with extensive knowledge sourced from both open-access and commercial databases, including: PubChem, ChEMBL, Google Patents, SciFinder and others. 

By leveraging these resources, we selected small molecules with potential high affinity and selectivity for the dark kinome targets. The integration of machine learning allowed for the prediction of compound efficacy and safety profiles, enhancing the efficiency of the drug discovery process.

For each of 10 kinase we provide list of compounds.