answer all the questions with explanation The following table is from Kumar et. al. Highly Selective Dopamine D3 Receptor (D3R) Antagonists andPartial Agonists Based on Eticlopride and the D3R Crystal Structure: New Leads for Opioid DependenceTreatment. J. Med Chem 2016.Table 1. Human D₁-Like Receptor Binding Data for Synthons"compdRABCD₂R11aHHOMea619 ± 97.6BCK± SEM (nM)D₁R446±25.2D,RD₂/D,D/D₁D₁/D₂2300 ± 8201.45.23.711bHClHH139±11.931.1 ± 0.462316 ± 47.14.S102.312aMeHOMeCl233±22.4179±18.1400 ± 83.41.32.21.712bMeClHH58.1 ± 3.0913.6 ± 0.48889.9 ± 6.814.36.61.513an-But13bn-ButHClOMeHC29.8 ± 4.5822.5 ± 4.86322±76.01.31411H2.93 + 0.3160.363 + 0.0526.5.1 + 10.08.117922"Binding inhibition values determined using HEK 293 cells transfected with hDR, hD,R, or hD and [H]N-methylspiperone radioligand asdescribed. 59a. What is meant by Ki?b. Which compound has the highest affinity for D₂R? (circle 1)11a12b13a13bc. Which compound is most selective for the D3R? (circle 1)11a13b

a. What is meant by Ki? Ki (inhibition constant) tells us how strongly a compound sticks to a…

Answered: The following table is from Kumar et.…

Organic Chemistry

8th Edition

ISBN:9781305580350

Author:William H. Brown, Brent L. Iverson, Eric Anslyn, Christopher S. Foote

Publisher:William H. Brown, Brent L. Iverson, Eric Anslyn, Christopher S. Foote

Chapter23: Amines

Section23.6: Reactions With Acids

Problem 23.9P

See similar textbooks

Similar questions

On the following page are three compounds, 1, 2, and 3, that have been investigated as anti-malarial candidates. Compound 1 is the "parent" molecule, and 2 and 3 are derivatives. Shown next to each molecule is (i) the enthalpy change when it binds to its target, and (ii) the dissociation constant for the molecule/target complex. Consider the structures and answer the following: AH = - 1.2 kcal/mol; Kp = 16 nM OH 1 HO AH = - 6.0 kcal/mol; Kp = 76 nM OH AH = - 5.5 kcal/mol; Kp = 0.5 nM OH 3 (i) What is the difference among 1, 2, and 3?
Example: Sulfacetamide degradation presents a pH-rate profile U-shaped. The first order constant in the pH independent zone (5-11) is 9 x 10-6 s-1 at 120° C. The activation energy is 22.9 kcal mol -1 at pH 7.4. Calculate the retest period at 25° C. R= 8,314 JK-¹mol-1 1 cal = 4,1868 J H₂N ZI
1. Do you expect the solubility of Borax to increase or decrease as temperature increases? Select the option that best explains why. ΔΗ A. Solubility will increase, because as Tincreases the therefore K will get larger. term becomes smaller RT ΔΗ B. Solubility will increase, because as Tincreases the term becomes smaller RT Choose... therefore Kwill get smaller. ΔΗ' C. Solubility will decrease, because as Tincreases the term becomes smaller RT therefore Kwill get smaller. ΔΗ' D. Solubility will decrease, because as Tincreases the term becomes smaller RT therefore Kwill get larger. 2. Why was it necessary to make sure that some solid was present in the main solution before taking the samples to measure Ksp? Select the option that best explains why. A. To make sure no more sodium borate would dissolve in solution. B. To ensure the dissolution process was at equilibrium. C. To make sure the solution was saturated with sodium and borate ions. Choose... D. All of the above
9. The following molecular tweezers bind 2,4,5,7-tetranitrofluorenone (TENF). The association constants for A, B, and Care 3.4 x 103,7.0 x 10°, and 1.7 × 10² M-1, respectively. Explain this trend. Meo Meo Meo OMe OMe OMe O,N NO, NO2 NO2 OMe OMe OMe TENF А. В. С.
Kk161.
Solving by condensation (Aldehydes and Ketones)
Calculate k, the degradation rate constant, responsible for drug degradation in this solution (in month-1).
Evaluate the synthetic model of a siderophore depicted below, designed to bind metal cations. Identify its strengths and weaknesses as a metal-binding agent. Propose an improved analogue with enhanced binding affinity for metals like Fe³⁺. Provide a detailed explanation for your suggestion(s), including considerations of solvent compatibility and solubility.
Calculate the value of the denaturation constant kd for a given enzyme, using the equation provided from the text and lecture of kd = Ad e(-Ed/RT) where Ad = 6.1 x 1047 and Ed = 69 kcal/g mole. Then, prepare a plot of per cent enzyme maximal activity vs temperature using an Ea of 23 kcal/gmole, and an enzyme concentration E0 of unity. Note that the y-axis of this plot is a per cent value, so the value of A in the Arrhenius equation does not need to be known in this case. On the denaturation side of the curve, use 5 minutes as the constant exposure time. Use a temperature range of 20 to 50⁰C.
In what way(s) might the results of the separation and purification procedureoutlined be different if the following conditions exist? Q. Aqueous NaOH is used in place of aqueous NaHCO3.
Molecule C below has a pka of 3.41 and D has a pKa of 3.47 i. Which molecule will be more deprotonated in a solution that has a pH of 3.45? Explain. ii. Use resonance/equilibria structures and explain the difference in pka. OH NO₂ C D OH
1. Alpha-glucosidase has a molar mass of about 40 kilodaltons. If 0.50 grams of the enzyme is dissolved in 250 mL of buffer, calculate Kcat for the enzyme with and without quercetin Note: Vmax for the reaction without quercetin = 0.6666 Vmax for the reaction with quercetin= 0.3333

SEE MORE QUESTIONS

Recommended textbooks for you

Organic Chemistry

Chemistry

ISBN:

9781305580350

Author:

William H. Brown, Brent L. Iverson, Eric Anslyn, Christopher S. Foote

Publisher:

Cengage Learning

EBK A SMALL SCALE APPROACH TO ORGANIC L

Chemistry

ISBN:

9781305446021

Author:

Lampman

Publisher:

CENGAGE LEARNING - CONSIGNMENT

Organic Chemistry

Chemistry

ISBN:

9781305580350

Author:

William H. Brown, Brent L. Iverson, Eric Anslyn, Christopher S. Foote

Publisher:

Cengage Learning

EBK A SMALL SCALE APPROACH TO ORGANIC L

Chemistry

ISBN:

9781305446021

Author:

Lampman

Publisher:

CENGAGE LEARNING - CONSIGNMENT

SEE MORE TEXTBOOKS