Therameutin Modulators

The method of claim 1, comprising administering a therapeutically effective amount of a compound having the formula V

• wherein:
• ring A is a 5-, 6-, or 7-membered ring or a 7- to 12-membered fused bicyclic ring;
• X1 is selected from N, N—R0 or C—R1;
• X2 is selected from N, N—R0 or C—R1;
• the dotted lines represent optional double bonds;
• each R1 is independently selected from the group consisting of H, alkyl, cycloalkyl, alkenyl,
• alkynyl, aralkyl, CN, CF3, NO2, OR11, —(CH2)pC(O)(CH2)qR11, —(CH2)pC(O)N(R12)(R13),
• —(CH2)pC(O)O(CH2)qR11, —(CH2)pN(R11)C(O)R11, —(CH2)pN(R12)(R13), —N(R11)SO2R11,
• —OC(O)N(R12)(R13), —SO2N(R12)(R13), halo, aryl, and a heterocyclic ring, and additionally or alternatively, two R1 groups on adjacent ring atoms form a 5- or 6-membered fused ring which contains from 0 to 3 heteroatoms;
• n is 0 to 6,
• each R11 is independently selected from H, alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl,
• aryl, and a heterocyclic ring;
• each R12 and R13 are independently selected from H, alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, aryl, and a heterocyclic ring;
• or R12 and R13 may be taken together with the nitrogen to which they are attached form a 5- to 7-membered ring which may optionally contain a further heteroatom;
• p is 0 to 4;
• q is 0 to 4;
• R22 is selected from H and C1-3 alkyl;
• R34 is selected from H, NO2, CN, alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, aryl and a heterocyclic ring;
• R55 is selected from H, alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, aryl, and a heterocyclic ring;
• R56 is selected from -Y″-R19;
• Y″ is selected from a chemical bond, O, NRO—, and a hydrocarbon chain having from 1 to 4 carbon atoms, and optionally substituted with one or more of halo, alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, CO2R0, C(O)R0, C(O)N(R0)2, CN, CF3, N(R0)2, NO2, and ORO;
• R19 is selected from the group consisting of H, alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, CF3, aryl, and a heterocyclic ring;
• and
• each R0 is independently selected from H, alkyl, cycloalkyl, aralkyl, aryl and a heterocyclic ring.

A method for determining whether a substance is an inhibitor or an activator of a theramutein which is capable of eliciting a detectable phenoresponse, which comprises:

• a) incubating a first cell which expresses the theramutein at a substantially constant level with the substance;
• b) incubating a second cell which expresses a corresponding prototheramutein at a substantially constant level with a known inhibitor or activator of the prototheramutein;
• c) comparing a phenoresponse of the second cell to the known inhibitor or activator of the prototheramutein to the phenoresponse of the first cell to the substance;
• and
• d) determining that the phenoresponse of the first cell is inhibited or activated to at least the same degree as the phenoresponse of the second cell is inhibited or activated by the known inhibitor or activator of the prototheramutein, thereby identifying the substance as an inhibitor or an activator of the theramutein.