describe lipinksi's rule of 5 (Ro5). which number is best similar or optimun drug like properties....

describe lipinksi's rule of 5 (Ro5). which number is best similar or optimun drug like properties.

and decribe PAINS.

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Expert Solution

Lipinksi's rule of five, also known as Rule of 5(Ro5) is basically a rule of thumb which is used to evaluate drug suitability or determine whether a chemical compound, with some certain pharmacological or biological activity, has the characteristics that would make it a orally active drug for human. The rule consists of...

1. Molecular weight should be less than 500 dalton

2. High lipophilicity i.e. octanol water partition coefficient (logP) should not exceed 5

3. There should be less than 5 hydrogen bond donors

4. There should be less than 10 hydrogen bond acceptors

5. Molar refractivity should be between 40-130

Here, we have seen that all the numbers are multiplication of 5. So the name of the rule.

PAINS: (pan assay interference compounds)

PAINS are prominent source of false in the drug discovery process. PAINS are biologically active compounds assembled as potential drug candidates during the high volume screening used to search for positive new drugs. PAINS work by interrupting the assay technology which is used in the screening to report biological activity. These drugs are not active against the intended biological target.

Some PAINS are: curcumin, phenolsulfonamides, enones, quinones cathechols etc.

queen_honey_blossom answered 2 years ago

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