Synonyms: Cosela® | G1T28
trilaciclib is an approved drug (FDA (2021))
Compound class:
Synthetic organic
Comment: Trilaciclib (G1T28) is a short-acting CDK4/6 inhibitor that was developed by G1 Therapeutics [2].
![]() Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
|
Bioactivity Comments |
Preclinical findings are reported in [1]. G1T28 is selective for CDK4/6 over other CDKs. Inhibition of off-target kinases with high affinity binding is reported- e.g. of the enzymes inhibited by >90% at 100nM G1T28, FLT3(D835V), GAK, NEK10, PRKD1, PRKD3, SNARK and ULK2 all have an affinity constant (Kd) <10nM [1]. |
Selectivity at enzymes | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | Click column headers to sort | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|