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Flashcards in Drug Discovery Deck (23)
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1
Q

Target (Protein)

A

The pathway (gene to protein to cell interaction) that results in some form of condition with clinical relevance. For example: the Renin-Angiotensin-Aldosterone-System

2
Q

Screening Assay

A

A cost effective method of screening multiple compounds to determine their compatibility with the Target.

3
Q

High Throughput Screening

A

The high volume testing of multiple varied compounds. These compounds could have been organic or synthetic in origin. Automated process.

4
Q

Hit

A

A compound identified through High Output Screening that succeeds in interacting with the Target.

5
Q

What are the four types of Bioassays?

A

Whole organism, mammalian cell cultures, purified enzymes or receptors, engineered microorganisms

6
Q

Lead Compound

A

The most successful of the Hits in the realm of toxicology and pharmacology

7
Q

Lead Optimization

A

Altering the Lead compound to maximize efficacy by modifying the binding of said drug

8
Q

Natural Products

A

A processed crude mixture of some material found in nature such that each of its many components are isolated for testing.

9
Q

Synthetic Compound Collections

A

Large collections of synthetically created compounds. They have limited structure options.

10
Q

Combinational Libraries

A

Large quantities of rapidly generated compounds made from chemical recombination. Libraries tailored to specific structures are the most successful of this concept.

11
Q

Virtual Libraries

A

A digital database of thousands of molecules that can be screens for molecular compatibility.

12
Q

Eutomer

A

A stereoisomer with the highest receptor afinity

13
Q

Distomer

A

A stereoisomer with the lowest receptor afinity

14
Q

Pharmacophore

A

The three dimensional arrangement of essential functional groups that cause a biological response. This is the minimum requirement for activity.

15
Q

Homologation

A

Adding similar constituents to a pharmacophore. Often varying lengths of one carbon structure.

16
Q

Chain Branching

A

Changing pharmacophores with different branching additions. Nitrogen and Carbon can both provide branches in this manner.

17
Q

Ring Transformation

A

Replacing structures of a pharmacophore until they form a ring structure. This requires two available locations for modification.

18
Q

Bioisostere (Classic)

A

Molecules or ions with the same number of atoms or the same numbers and arrangements of valence electrons.

19
Q

Bioisostere (Non-classical)

A

Groups of atoms with similar chemical or physical properties.

20
Q

QSAR

A

Quantitative Structure Activity Relationships. The mathematical models that predict the viability between a drug and a receptor.

21
Q

Log P

A

The measure of Lipophilicy which is relevant for QSAR. It is the ratio of the drug’s concentration in Octanol and concentration in Water.

22
Q

Water soluble (Log P)

A

A Log P value of 0.5 or less indicates it is water soluble.

23
Q

Lipinski’s Rule of Five

A

Four broad rules that indicate a good drug molecule: 1. MW